Entinostat (MS-275)

別名：SNDX-275

製品コード：S1053 純度：99.96%

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.

CAS No. 209783-80-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 74500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（394）

製品安全説明書

現在のバッチを見る：純度： 99.96%

99.96

Entinostat (MS-275)と併用されることが多い化合物

Quisinostat (JNJ-26481585) 2HCl

Entinostat and Quisinostat 2HCl are HDAC inhibitors that prevent CaMKII overexpression-induced cardiac myocyte hypertrophy.

Zhang M, et al. J Mol Cell Cardiol. 2020 Dec;149:73-81.

Entinostat (MS-275)関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
関連製品	TSA (Trichostatin A) Mocetinostat (MGCD0103) RGFP966 Tubastatin A Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) 2HCl MC1568 Tubastatin A HCl PCI-34051 Tacedinaline (CI994) LMK-235 Fimepinostat (CUDC-907) Tubacin Givinostat (ITF2357) TMP269 AR-42 Sodium butyrate Pracinostat (SB939) Santacruzamate A (CAY10683) Abexinostat (PCI-24781) (-)-Parthenolide CUDC-101 Dacinostat (LAQ824) CAY10603 RG2833 (RGFP109) Tasquinimod Tucidinostat (Chidamide) TMP195 Nexturastat A Droxinostat Domatinostat (4SC-202) Scriptaid 4-PBA (4-Phenylbutyric acid) M344 Resminostat Citarinostat (ACY-241) BG45 WT161 ACY-738 HPOB ITSA-1 (ITSA1) Tubastatin A TFA TC-H 106 SIS17 ACY-775 BML-210 (CAY10433) TH34 Raddeanin A	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
U937	Function assay	5 uM	24 hrs	Increase in histone H3 acetylation in U937 cells at 5 uM after 24 hrs by Western blot analysis.	17447750
HCT116	Function assay	10 uM	24 hrs	Inhibition of HDAC1 in human HCT116 cells assessed as induction of hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis.	20452226
NB4	Cell cycle arrest assay	5 uM	24 hrs	Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis.	20491440
NB4	Function assay	5 uM	24 hrs	Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis.	20491440
epithelial cells	Function assay	1 uM	4, 6, and 8 days	Inhibition of HDAC7 in human homozygous Fdelta508 primary bronchial epithelial cells assessed as increase in short circuit currents at 1 uM for 4, 6, and 8 days relative to control.	19966789
Hela	Function assay	0.6 uM	16 hrs	Inhibition of HDAC6 in human Hela cells assessed as increase in total lysine acetylation at 0.6 uM after 16 hrs by immunofluorescence microscopy.	21696956
U937	Cell cycle arrest assay	5 uM	30 hrs	Cell cycle arrest in human U937 cells assessed as accumulation at G1 phase at 5 uM after 30 hrs by propidium iodide staining based flow cytometry.	21215647
NB4	Function assay	5 uM	24 hrs	Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis.	20491440
C127-LT	Function assay	1 uM	24 hrs	Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 1 uM after 24 hrs by fluorescence microscopy.	26996372
C127-LT	Function assay	10 uM	24 hrs	Inhibition of HDAC in mouse C127-LT cells assessed as activation of EGFP expression at 10 uM after 24 hrs by fluorescence microscopy.	26996372
HCT116	Function assay	10 uM	24 hrs	Inhibition of HDAC2 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis.	22321215
HCT116	Function assay	10 uM	24 hrs	Inhibition of HDAC1 in human HCT116 cells assessed as hyperacetylation of histone H3 at 10 uM after 24 hrs by Western blot analysis.	22321215
HeLa	Function assay	1 uM	6 hrs	Inhibition of HDAC1/HDAC2/HDAC3 in human HeLa cells assessed as increase in intracellular acetyl-histone H4 levels at 1 uM after 6 hrs by Western blot analysis.	29787262
MV4-11	Apoptosis assay	5 uM	24 to 48 hrs	Induction of apoptosis in human MV4-11 cells at 5 uM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry.	29738953
MV4-11	Function assay	200 nM	24 hrs	Inhibition of class 1 HDAC in human MV4-11 cells assessed as hyperacetylation of histone H3 at 200 nM after 24 hrs by Western blot analysis.	29738953
HL60	Apoptosis assay	5 uM	48 hrs	Induction of apoptosis in human HL60 cells assessed as decrease in procaspase-3 level at 5 uM after 48 hrs by Western blot analysis.	28415009
HL60	Apoptosis assay	5 uM	48 hrs	Induction of apoptosis in human HL60 cells assessed as increase in cleaved caspase-3 level at 5 uM after 48 hrs by Western blot analysis.	28415009
HL60	Apoptosis assay	5 uM	48 hrs	Induction of apoptosis in human HL60 cells assessed as increase in cleaved PARP level at 5 uM after 48 hrs by Western blot analysis.	28415009
MV4-11	Cell cycle arrest assay	5 uM	24 hrs	Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method.	29589441
HEL	Cell cycle arrest assay	5 uM	24 hrs	Cell cycle arrest in human HEL cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method.	29589441
Jurkat	Cell cycle arrest assay	5 uM	24 hrs	Cell cycle arrest in human Jurkat cells at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method.	29589441
MV4-11	Function assay	5 uM	24 hrs	Inhibition of class 1 HDAC in human MV4-11 cells assessed as induction of histone hyperacetylation at 5 uM after 24 hrs by Western blot method.	29589441
LNCAP	Function assay	10 uM	24 hrs	Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation at 10 uM measured after 24 hrs relative to control.	27717544
epithelial cells	Function assay	5 uM		Inhibition of HDAC in human primary bronchial epithelial cells assessed as induction of mutant Fdelta508 CFTR protein apical surface localization at 5 uM.	19966789
HCT116	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 0.1 μM.	22705022
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1 μM.	22705022
SK-N-BE(2)	Antiproliferative assay		48 hrs	Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.33 μM.	28511906
AGS	Antiproliferative assay		72 hrs	Antiproliferative activity against human AGS cells after 72 hrs by MTT assay, IC50 = 0.34 μM.	29787262
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells treated for 48 hrs followed by refreshed every 96 hrs measured on day 10 by Lowry assay, IC50 = 0.35 μM.	26613635
HEL	Function assay		3 hrs	Inhibition of class 1 HDAC in HEL cells using Boc-Lys (acetyl)-AMC as substrate preincubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.43 μM.	28511906
PC3	Growth inhibition assay		48 hrs	Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay, GI50 = 0.43 μM.	28395150
HEL	Antiproliferative assay		72 hrs	Antiproliferative activity against human HEL cells after 72 hrs by MTT assay, IC50 = 0.44 μM.	29787262
MOLT4	Antiproliferative assay		72 hrs	Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay, IC50 = 0.45 μM.	29787262
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay, IC50 = 0.47 μM.	29202397
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 0.48 μM.	28511906
U937	Antiproliferative assay		72 hrs	Antiproliferative activity against human U937 cells incubated for 72 hrs by MTT assay, IC50 = 0.55 μM.	25953722
U937	Antiproliferative assay		72 hrs	Antiproliferative activity against human U937 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.55 μM.	25874326
HCT116	Growth inhibition assay		2 days	Growth inhibition of human HCT116 cells after 2 days by MTT assay, GI50 = 0.6 μM.	22541394
HL60	Function assay		3 hrs	Inhibition of class 1 HDAC in human HL60 cells using Boc-Ac-Lys-AMC as substrate incubated for 3 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 0.62 μM.	28415009
MOLT4	Antiproliferative assay		48 hrs	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.65 μM.	28511906
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human P53 expressing HCT116 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 0.7 μM.	19441846
HEK293T	Function assay		1 hr	Inhibition of FLAG-tagged HDAC2 (unknown origin) expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 0.74 μM.	29289885
HCT116	Antiproliferative assay		3 days	Antiproliferative activity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.76 μM.	22321215
U937	Antiproliferative assay		48 hrs	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay, IC50 = 0.77 μM.	28415009
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 0.78 μM.	25874326
K562	Function assay		10 mins	Inhibition of KDAC3 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 0.79 μM.	26681404
HCT116	Cytotoxicity assay		3 days	Cytotoxicity against human HCT116 cells after 3 days by WST-1 assay, IC50 = 0.8 μM.	20452226
Sf9	Function assay		3 hrs	Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins by fluorometric method, IC50 = 0.9 μM.	28501514
HEK293T	Function assay		1 hr	Inhibition of human FLAG-tagged HDAC1 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.07 μM.	29289885
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human P53 expressing A549 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.2 μM.	19441846
HEK293T	Function assay		1 hr	Inhibition of human FLAG-tagged HDAC3 expressed in HEK293T cells using acetylated lysine side chain as substrate after 1 hr by colorimetric detection based assay, IC50 = 1.23 μM.	29289885
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against HEL cells after 48 hrs by MTT assay, IC50 = 1.29 μM.	28415009
G401	Antiproliferative assay		72 hrs	Antiproliferative activity against human G401 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.3 μM.	19441846
Sf9	Function assay		3 hrs	Inhibition of recombinant C-terminal His-tagged HDAC11 (unknown origin) expressed in baculovirus infected Sf9 cells using Ac-Arg-Gly-Lys(Ac)-AMC as substrate pretreated for 3 hrs followed by substrate addition after 30 mins in presence of 0.2 uM SAHA by f, IC50 = 1.3 μM.	28501514
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.32 μM.	28511906
Huh7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 1.4 μM.	25490700
MDA-MB-231	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.41 μM.	28395150
K562	Function assay		10 mins	Inhibition of KDAC1 in human K562 cells using [3H]acetylated histone as substrate incubated for 10 mins by liquid scintillation counting method, IC50 = 1.48 μM.	26681404
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 1.52 μM.	28415009
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay, IC50 = 1.6 μM.	29202397
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.68 μM.	28415009
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human P53-deficient HeLa cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 1.8 μM.	19441846
HCT116	Function assay		18 hrs	Inhibition of HDAC in human HCT116 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 1.96 μM.	28340413
HCT116	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.03 μM.	28340413
HCT116	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 2.07 μM.	28415009
NCI-H661	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H661 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 2.19 μM.	25874326
NCI-H661	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H661 cells incubated for 72 hrs by MTT assay, IC50 = 2.19 μM.	25953722
Sf9	Function assay		17 hrs	Inhibition of His6-tagged HDAC3/SMRT (395 to 489 residues) (unknown origin) co-expressed in baculovirus infected sf9 cells using (FAM)-labeled acetylated peptide substrate after 17 hrs by caliper microfluidic mobility shift assay, IC50 = 2.31206 μM.	30179749
ACHN	Antiproliferative assay		72 hrs	Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2.4 μM.	29787262
SGC7901	Growth inhibition assay		72 hrs	Growth inhibition of human SGC7901 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 2.5 μM.	23061376
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 2.55 μM.	29787262
MDA-MB-231	Anticancer assay		72 hrs	Anticancer activity against human MDA-MB-231 cells after 72 hrs by MTT assay, GI = 2.8 μM.	21741834
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by celltiter-blue cell viability assay, CC50 = 3 μM.	19441846
HCT116	Anticancer assay		72 hrs	Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, GI = 3.1 μM.	21741834
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50 = 3.1 μM.	29787262
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 3.11 μM.	28340413
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 3.134 μM.	26140961
A2780	Function assay		18 hrs	Inhibition of HDAC in human A2780 cells using Boc-Lys (epsilon-Ac)-AMC as substrate pretreated for 18 hrs followed by substrate addition after 3 hrs by fluorescence assay, IC50 = 3.15 μM.	28340413
HeLa	Function assay		30 mins	Inhibition of human HDAC in HeLa cells after 30 mins by Fluor de Lys fluorescence assay, IC50 = 3.2 μM.	21889343
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 3.66 μM.	29787262
A375	Antiproliferative assay		72 hrs	Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay, IC50 = 3.67 μM.	29202397
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 4.02 μM.	28340413
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50 = 4.53 μM.	28340413
MDA-MB-231	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 4.63 μM.	25874326
MGC803	Antiproliferative assay		72 hrs	Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay, IC50 = 4.89 μM.	29202397
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 4.89 μM.	28511906
HuH7	Cytotoxicity assay		3 days	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 5.1 μM.	25490700
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 5.1 μM.	26140961
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT-based assay, IC50 = 5.41 μM.	25874326
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay, IC50 = 5.41 μM.	25953722
A2780	Anticancer assay		72 hrs	Anticancer activity against human A2780 cells after 72 hrs by MTT assay, GI = 5.7 μM.	21741834
A549	Growth inhibition assay		48 hrs	Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay, GI50 = 5.76 μM.	28395150
A2780	Antiproliferative assay		48 hrs	Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay, IC50 = 5.89 μM.	28340413
SMMC7721	Antiproliferative assay		72 hrs	Antiproliferative activity against human SMMC7721 cells after 72 hrs by CCK-8 assay, IC50 = 5.97 μM.	29202397
U266	Antiproliferative assay		48 hrs	Antiproliferative activity against human U266 cells after 48 hrs by MTT assay, IC50 = 6.1 μM.	28415009
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 6.36 μM.	28340413
U251	Growth inhibition assay		2 days	Growth inhibition of human U251 cells after 2 days by MTT assay, GI50 = 6.5 μM.	22541394
NCI-H1299	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay, IC50 = 6.74 μM.	29202397
AsPC1	Growth inhibition assay		48 hrs	Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay, GI50 = 6.9 μM.	28395150
BGC823	Growth inhibition assay		72 hrs	Growth inhibition of human BGC823 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 7.1 μM.	23061376
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 7.881 μM.	26140961
DU145	Anticancer assay		72 hrs	Anticancer activity against human DU145 cells after 72 hrs by MTT assay, GI = 7.9 μM.	21741834
Bel7402	Growth inhibition assay		72 hrs	Growth inhibition of human Bel7402 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8 μM.	23061376
HeLa	Function assay		20 mins	Inhibition of HDAC in human HeLa cells using fluor de Lys as substrate incubated for 20 mins by microplate spectrofluorometric analysis, IC50 = 8.02 μM.	27060764
MGC803	Growth inhibition assay		72 hrs	Growth inhibition of human MGC803 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 8.9 μM.	23061376
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, GI50 = 9.32 μM.	28629630
SMMC7721	Growth inhibition assay		72 hrs	Growth inhibition of human SMMC7721 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 11 μM.	23061376
HeLa	Function assay		24 to 48 hrs	Inhibition of HDAC in human HeLa cells using Boc-Lys(AC)-AMC as substrate after 24 to 48 hrs by spectrofluorometry, IC50 = 11.18 μM.	26996372
SKHEP1	Growth inhibition assay		72 hrs	Growth inhibition of human SKHEP1 cells incubated for 72 hrs by WST dye reduction assay, GI90 = 13 μM.	23061376
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50 = 18.37 μM.	28629630
PC3	Antiproliferative assay		48 hrs	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, GI50 = 19.09 μM.	28629630
HeLa	Antiproliferative assay		48 hrs	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50 = 19.24 μM.	28629630
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, GI50 = 19.26 μM.	28629630
HCT116	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 27.47 μM.	18701301
U251	Growth inhibition assay		2 days	Growth inhibition of human U251 cells after 2 days by MTT assay, TGI = 40 μM.	22541394
HEK293 STF	Function assay		24 hrs	Activation of mouse Wnt3a signaling expressed in HEK293 STF cells assessed as increase in transcriptional activity after 24 hrs by luciferase reporter gene-based lactate dehydrogenase assay.	19022675
A4-Fuk	Growth Inhibition Assay			IC50=1.15364 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=1.13165 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=1.12007 μM	SANGER
PF-382	Growth Inhibition Assay			IC50=1.11513 μM	SANGER
L-540	Growth Inhibition Assay			IC50=1.10604 μM	SANGER
TGW	Growth Inhibition Assay			IC50=1.07675 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=1.03454 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=1.0241 μM	SANGER
HH	Growth Inhibition Assay			IC50=0.98959 μM	SANGER
SK-PN-DW	Growth Inhibition Assay			IC50=0.97831 μM	SANGER
DMS-153	Growth Inhibition Assay			IC50=0.97469 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=0.9683 μM	SANGER
ES6	Growth Inhibition Assay			IC50=0.96437 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=0.95901 μM	SANGER
GOTO	Growth Inhibition Assay			IC50=0.95076 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=0.93284 μM	SANGER
EHEB	Growth Inhibition Assay			IC50=0.92585 μM	SANGER
GDM-1	Growth Inhibition Assay			IC50=0.88687 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=0.88096 μM	SANGER
ST486	Growth Inhibition Assay			IC50=0.87917 μM	SANGER
JAR	Growth Inhibition Assay			IC50=0.87827 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=0.87171 μM	SANGER
ES4	Growth Inhibition Assay			IC50=0.85868 μM	SANGER
BL-70	Growth Inhibition Assay			IC50=0.85702 μM	SANGER
LC4-1	Growth Inhibition Assay			IC50=0.84007 μM	SANGER
CESS	Growth Inhibition Assay			IC50=0.81197 μM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=0.81084 μM	SANGER
CPC-N	Growth Inhibition Assay			IC50=0.80524 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=0.80147 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=0.7836 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=0.78308 μM	SANGER
Daudi	Growth Inhibition Assay			IC50=0.77681 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=0.77567 μM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=0.77348 μM	SANGER
SW954	Growth Inhibition Assay			IC50=0.75999 μM	SANGER
CCRF-CEM	Growth Inhibition Assay			IC50=0.74661 μM	SANGER
NB14	Growth Inhibition Assay			IC50=0.72617 μM	SANGER
COR-L279	Growth Inhibition Assay			IC50=0.70996 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=0.70492 μM	SANGER
ECC12	Growth Inhibition Assay			IC50=0.70086 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=0.68343 μM	SANGER
NB13	Growth Inhibition Assay			IC50=0.66817 μM	SANGER
SU-DHL-1	Growth Inhibition Assay			IC50=0.65947 μM	SANGER
CW-2	Growth Inhibition Assay			IC50=0.65794 μM	SANGER
NALM-6	Growth Inhibition Assay			IC50=0.6486 μM	SANGER
KE-37	Growth Inhibition Assay			IC50=0.64276 μM	SANGER
NCI-H526	Growth Inhibition Assay			IC50=0.63541 μM	SANGER
LOUCY	Growth Inhibition Assay			IC50=0.63364 μM	SANGER
LU-165	Growth Inhibition Assay			IC50=0.61812 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=0.60719 μM	SANGER
NB69	Growth Inhibition Assay			IC50=0.59825 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=0.58703 μM	SANGER
KARPAS-299	Growth Inhibition Assay			IC50=0.58504 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=0.58242 μM	SANGER
SIG-M5	Growth Inhibition Assay			IC50=0.57848 μM	SANGER
LU-134-A	Growth Inhibition Assay			IC50=0.57073 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=0.56889 μM	SANGER
L-363	Growth Inhibition Assay			IC50=0.56657 μM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=0.56105 μM	SANGER
NCI-H524	Growth Inhibition Assay			IC50=0.55401 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=0.55306 μM	SANGER
NB17	Growth Inhibition Assay			IC50=0.5438 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=0.54261 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=0.53663 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=0.53041 μM	SANGER
HCC1599	Growth Inhibition Assay			IC50=0.5157 μM	SANGER
ACN	Growth Inhibition Assay			IC50=0.51028 μM	SANGER
HC-1	Growth Inhibition Assay			IC50=0.50473 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=0.49661 μM	SANGER
NCI-H187	Growth Inhibition Assay			IC50=0.49227 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=0.48358 μM	SANGER
K5	Growth Inhibition Assay			IC50=0.47025 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=0.44501 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=0.43897 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=0.43453 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=0.43403 μM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=0.43153 μM	SANGER
OPM-2	Growth Inhibition Assay			IC50=0.41513 μM	SANGER
RPMI-6666	Growth Inhibition Assay			IC50=0.4112 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=0.41017 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=0.40613 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=0.40367 μM	SANGER
SCH	Growth Inhibition Assay			IC50=0.40342 μM	SANGER
A101D	Growth Inhibition Assay			IC50=0.403 μM	SANGER
CHP-126	Growth Inhibition Assay			IC50=0.40231 μM	SANGER
SK-MM-2	Growth Inhibition Assay			IC50=0.39868 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay			IC50=0.38776 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=0.38701 μM	SANGER
NCCIT	Growth Inhibition Assay			IC50=0.38649 μM	SANGER
ARH-77	Growth Inhibition Assay			IC50=0.38193 μM	SANGER
DEL	Growth Inhibition Assay			IC50=0.37487 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=0.37121 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=0.36935 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=0.3673 μM	SANGER
ES8	Growth Inhibition Assay			IC50=0.36022 μM	SANGER
CMK	Growth Inhibition Assay			IC50=0.35727 μM	SANGER
SR	Growth Inhibition Assay			IC50=0.34261 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=0.3381 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay			IC50=0.33716 μM	SANGER
LU-139	Growth Inhibition Assay			IC50=0.3351 μM	SANGER
NB12	Growth Inhibition Assay			IC50=0.31756 μM	SANGER
HEL	Growth Inhibition Assay			IC50=0.31348 μM	SANGER
ATN-1	Growth Inhibition Assay			IC50=0.30576 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=0.30256 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=0.28708 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=0.27833 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=0.24079 μM	SANGER
COR-L88	Growth Inhibition Assay			IC50=0.22959 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=0.20113 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=0.19619 μM	SANGER
SF539	Growth Inhibition Assay			IC50=0.19593 μM	SANGER
A3-KAW	Growth Inhibition Assay			IC50=0.17627 μM	SANGER
CRO-AP2	Growth Inhibition Assay			IC50=0.16889 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=0.13527 μM	SANGER
NCI-H1417	Growth Inhibition Assay			IC50=0.12974 μM	SANGER
NCI-H1963	Growth Inhibition Assay			IC50=0.11579 μM	SANGER
ES1	Growth Inhibition Assay			IC50=0.11255 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=0.10912 μM	SANGER
NCI-H748	Growth Inhibition Assay			IC50=0.10334 μM	SANGER
697	Growth Inhibition Assay			IC50=0.09976 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=0.06355 μM	SANGER
SCC-3	Growth Inhibition Assay			IC50=0.061 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=1.16641 μM	SANGER
HAL-01	Growth Inhibition Assay			IC50=1.16943 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=1.17659 μM	SANGER
NCI-H719	Growth Inhibition Assay			IC50=1.17898 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=1.18114 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=1.20266 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=1.21489 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=1.22118 μM	SANGER
no-10	Growth Inhibition Assay			IC50=1.23112 μM	SANGER
MHH-CALL-2	Growth Inhibition Assay			IC50=1.24721 μM	SANGER
SK-N-DZ	Growth Inhibition Assay			IC50=1.24776 μM	SANGER
SCLC-21H	Growth Inhibition Assay			IC50=1.26478 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=1.27425 μM	SANGER
NB1	Growth Inhibition Assay			IC50=1.27732 μM	SANGER
NCI-H64	Growth Inhibition Assay			IC50=1.28462 μM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay			IC50=1.28577 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=1.28663 μM	SANGER
8-MG-BA	Growth Inhibition Assay			IC50=1.28866 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=1.29947 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=1.30998 μM	SANGER
CAL-148	Growth Inhibition Assay			IC50=1.32542 μM	SANGER
NCI-H2171	Growth Inhibition Assay			IC50=1.34502 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay			IC50=1.3539 μM	SANGER
NCI-H2107	Growth Inhibition Assay			IC50=1.35883 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=1.38978 μM	SANGER
K-562	Growth Inhibition Assay			IC50=1.39219 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=1.42287 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=1.42691 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=1.42741 μM	SANGER
MC116	Growth Inhibition Assay			IC50=1.43615 μM	SANGER
KARPAS-422	Growth Inhibition Assay			IC50=1.45358 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=1.47103 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=1.47987 μM	SANGER
BT-474	Growth Inhibition Assay			IC50=1.51764 μM	SANGER
A388	Growth Inhibition Assay			IC50=1.51945 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=1.5226 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=1.53564 μM	SANGER
KM-H2	Growth Inhibition Assay			IC50=1.5667 μM	SANGER
GR-ST	Growth Inhibition Assay			IC50=1.5682 μM	SANGER
RPMI-8866	Growth Inhibition Assay			IC50=1.60144 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=1.61901 μM	SANGER
NCI-H82	Growth Inhibition Assay			IC50=1.63406 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=1.63459 μM	SANGER
KM12	Growth Inhibition Assay			IC50=1.647 μM	SANGER
NB5	Growth Inhibition Assay			IC50=1.65677 μM	SANGER
HDLM-2	Growth Inhibition Assay			IC50=1.68281 μM	SANGER
KU812	Growth Inhibition Assay			IC50=1.69605 μM	SANGER
DB	Growth Inhibition Assay			IC50=1.70353 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=1.75234 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=1.77207 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=1.78879 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=1.79388 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=1.79508 μM	SANGER
ES7	Growth Inhibition Assay			IC50=1.80302 μM	SANGER
SW872	Growth Inhibition Assay			IC50=1.81395 μM	SANGER
TK10	Growth Inhibition Assay			IC50=1.83108 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=1.83563 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=1.84422 μM	SANGER
MLMA	Growth Inhibition Assay			IC50=1.88234 μM	SANGER
D-542MG	Growth Inhibition Assay			IC50=1.89373 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=1.9272 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=1.9328 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=1.93866 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=2.00262 μM	SANGER
LAN-6	Growth Inhibition Assay			IC50=2.01966 μM	SANGER
NCI-H510A	Growth Inhibition Assay			IC50=2.04502 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=2.05124 μM	SANGER
HT	Growth Inhibition Assay			IC50=2.10454 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=2.11482 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=2.11792 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=2.16873 μM	SANGER
NCI-H1522	Growth Inhibition Assay			IC50=2.21723 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=2.26902 μM	SANGER
DG-75	Growth Inhibition Assay			IC50=2.27148 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=2.32855 μM	SANGER
SF126	Growth Inhibition Assay			IC50=2.33094 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=2.33145 μM	SANGER
NCI-H345	Growth Inhibition Assay			IC50=2.33277 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=2.34936 μM	SANGER
NB10	Growth Inhibition Assay			IC50=2.41092 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=2.42267 μM	SANGER
CP66-MEL	Growth Inhibition Assay			IC50=2.4777 μM	SANGER
L-428	Growth Inhibition Assay			IC50=2.48521 μM	SANGER
DMS-79	Growth Inhibition Assay			IC50=2.54103 μM	SANGER
NCI-H1882	Growth Inhibition Assay			IC50=2.67562 μM	SANGER
KGN	Growth Inhibition Assay			IC50=2.76876 μM	SANGER
EW-1	Growth Inhibition Assay			IC50=2.77083 μM	SANGER
U-266	Growth Inhibition Assay			IC50=2.84823 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay			IC50=2.85641 μM	SANGER
KMOE-2	Growth Inhibition Assay			IC50=2.87711 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=2.9248 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=2.92957 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=3.00511 μM	SANGER
NCI-H2227	Growth Inhibition Assay			IC50=3.02079 μM	SANGER
U-87-MG	Growth Inhibition Assay			IC50=3.03513 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=3.05206 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=3.05376 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=3.14378 μM	SANGER
NCI-H2141	Growth Inhibition Assay			IC50=3.16566 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=3.18279 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=3.21342 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=3.43659 μM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=3.45227 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=3.46589 μM	SANGER
SF268	Growth Inhibition Assay			IC50=3.48174 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=3.51699 μM	SANGER
NB6	Growth Inhibition Assay			IC50=3.55563 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=3.59899 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=3.61624 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=3.62671 μM	SANGER
NCI-H1155	Growth Inhibition Assay			IC50=3.70947 μM	SANGER
RKO	Growth Inhibition Assay			IC50=3.77189 μM	SANGER
ECC4	Growth Inhibition Assay			IC50=3.97195 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=3.97547 μM	SANGER
EB-3	Growth Inhibition Assay			IC50=3.99633 μM	SANGER
SHP-77	Growth Inhibition Assay			IC50=4.00524 μM	SANGER
NCI-H2196	Growth Inhibition Assay			IC50=4.05625 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=4.06399 μM	SANGER
MN-60	Growth Inhibition Assay			IC50=4.1087 μM	SANGER
NCI-H1694	Growth Inhibition Assay			IC50=4.13405 μM	SANGER
LU-65	Growth Inhibition Assay			IC50=4.15332 μM	SANGER
NCI-H1436	Growth Inhibition Assay			IC50=4.18333 μM	SANGER
KINGS-1	Growth Inhibition Assay			IC50=4.31432 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=4.33268 μM	SANGER
Becker	Growth Inhibition Assay			IC50=4.37312 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=4.89657 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=5.00416 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=5.13778 μM	SANGER
NB7	Growth Inhibition Assay			IC50=5.14112 μM	SANGER
SW962	Growth Inhibition Assay			IC50=5.38814 μM	SANGER
no-11	Growth Inhibition Assay			IC50=5.76343 μM	SANGER
KNS-81-FD	Growth Inhibition Assay			IC50=5.90694 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=5.99494 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=6.08895 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=6.2851 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=6.42623 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=6.46321 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=6.67557 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=6.92301 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=8.13166 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=8.27786 μM	SANGER
EW-12	Growth Inhibition Assay			IC50=8.40803 μM	SANGER
A253	Growth Inhibition Assay			IC50=8.84661 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=8.89319 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=8.99042 μM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=9.17746 μM	SANGER
WSU-NHL	Growth Inhibition Assay			IC50=9.77478 μM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=9.97904 μM	SANGER
SK-LMS-1	Growth Inhibition Assay			IC50=10.2834 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=10.5924 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=11.6004 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=11.7682 μM	SANGER
NCI-H2081	Growth Inhibition Assay			IC50=11.7786 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=12.2463 μM	SANGER
CAS-1	Growth Inhibition Assay			IC50=12.3631 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=12.6131 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=12.7952 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=12.8013 μM	SANGER
LS-1034	Growth Inhibition Assay			IC50=14.3975 μM	SANGER
EW-18	Growth Inhibition Assay			IC50=14.448 μM	SANGER
Raji	Growth Inhibition Assay			IC50=14.5049 μM	SANGER
D-283MED	Growth Inhibition Assay			IC50=14.6271 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=14.9696 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay			IC50=15.4633 μM	SANGER
P30-OHK	Growth Inhibition Assay			IC50=17.7831 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=19.0186 μM	SANGER
NCI-H1395	Growth Inhibition Assay			IC50=20.6703 μM	SANGER
U-698-M	Growth Inhibition Assay			IC50=20.7075 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=20.7223 μM	SANGER
SW684	Growth Inhibition Assay			IC50=21.1716 μM	SANGER
NCI-H716	Growth Inhibition Assay			IC50=21.3154 μM	SANGER
JVM-2	Growth Inhibition Assay			IC50=21.4133 μM	SANGER
NCI-H1581	Growth Inhibition Assay			IC50=22.4148 μM	SANGER
CA46	Growth Inhibition Assay			IC50=31.6936 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=33.6503 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=35.9624 μM	SANGER
TUR	Growth Inhibition Assay			IC50=36.0521 μM	SANGER
REH	Growth Inhibition Assay			IC50=37.8211 μM	SANGER
EW-22	Growth Inhibition Assay			IC50=42.2885 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=42.7853 μM	SANGER
ES3	Growth Inhibition Assay			IC50=43.1339 μM	SANGER
EW-11	Growth Inhibition Assay			IC50=44.8218 μM	SANGER
RH-1	Growth Inhibition Assay			IC50=47.5812 μM	SANGER
HepG2	Function assay			Inhibition of human HepG2 cells, IC50 = 0.0009 μM.	18247554
HEK293	Function assay			Inhibition of human C-terminal FLAG-tagged HDAC1 in HEK293 cells, IC50 = 0.12 μM.	19441846
HEK293	Function assay			Inhibition of HDAC1 in HEK293 cells, IC50 = 0.12 μM.	18308563
SNU16	Function assay			Inhibition of HDAC from human SNU16 cells, IC50 = 0.233 μM.	18247554
HEK293	Function assay			Inhibition of human C-terminal FLAG-tagged HDAC2 in HEK293 cells, IC50 = 0.25 μM.	19441846
U937	Function assay			Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay, IC50 = 0.3 μM.	18381238
HEK293	Function assay			Inhibition of human C-terminal FLAG-tagged HDAC3 in HEK293 cells, IC50 = 0.4 μM.	19441846
HEK293	Function assay			Inhibition of HDAC3 in HEK293 cells, IC50 = 0.4 μM.	18308563
HCT116	Function assay			Inhibition of human HCT116 cells, IC50 = 0.5 μM.	18247554
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells, IC50 = 0.67 μM.	21742496
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.67 μM.	21650221
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by CellTiter-Blue cell viability assay, IC50 = 0.7 μM.	18370373
ML1	Antitumor assay			Antitumor activity against mouse ML1 cells, IC50 = 0.75 μM.	19534534
SKBR3	Antiproliferative assay			Antiproliferative activity against human SKBR3 cells, IC50 = 0.87 μM.	18247554
S2	Function assay			Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.94 μM.	19317450
A549	Antiproliferative assay			Antiproliferative activity against human A549 cells by CellTiter-Blue cell viability assay, IC50 = 1.2 μM.	18370373
G401	Antiproliferative assay			Antiproliferative activity against human G401 cells by CellTiter-Blue cell viability assay, IC50 = 1.3 μM.	18370373
HeLa	Antiproliferative assay			Antiproliferative activity against HeLa cells by alamar blue assay, IC50 = 1.58489 μM.	17606370
HeLa	Antiproliferative assay			Antiproliferative activity against human HeLa cells by CellTiter-Blue cell viability assay, IC50 = 1.8 μM.	18370373
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells by MTT assay, IC50 = 2 μM.	19131248
K562	Function assay			Inhibition of human histone deacetylase (mixture of HDAC1 and HDAC2) prepared from K562 erythroleukemia cells., IC50 = 2 μM.	12419380
K562	Function assay			Inhibitory activity against Histone deacetylase (HDAC) in K 562 erythroleukemia cells, IC50 = 2 μM.	14592473
SNU-16	Function assay			Inhibitory activity against Histone deacetylase (HDAC) from SNU-16 (human gastric adenocarcinoma) cells, IC50 = 2.19459 μM.	14667227
A2780	Antiproliferative assay			Antiproliferative activity against human A2780 cells by CellTiter-Blue cell viability assay, IC50 = 3 μM.	18370373
SW620	Function assay			Inhibition of human SW620 cells, IC50 = 3.2 μM.	18247554
A549	Antiproliferative assay			Antiproliferative activity against human A549 cells, IC50 = 3.58 μM.	18247554
MKN45	Antiproliferative assay			Antiproliferative activity against human MKN45 cells, IC50 = 4.16 μM.	18247554
MCF7	Function assay			Inhibition of human MCF7 cells, IC50 = 4.3 μM.	18247554
K562	Function assay			Inhibitory activity against partially purified histone deacetylase of human leukemia K562 cells., IC50 = 4.8 μM.	10425110
HeLa	Function assay			Inhibition of HDAC from human HeLa cells assessed as of histone H3 acetylation, IC50 = 4.8 μM.	19534534
HeLa	Function assay			Inhibition of HDAC in HeLa cells, IC50 = 12.5892 μM.	17606370
U937	Function assay			Inhibition of human HDAC1 in U937 cells by immunoprecipitation assay.	18381238
U937	Function assay			Induction of histone H4 hyperacetylation in human U937 cells.	18381238
U937	Function assay			Inhibition of human HDAC4 in U937 cells by immunoprecipitation assay.	18381238
U937	Function assay			Induction of granulocytic differentiation in human U937 cells.	18381238
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells.	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells.	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells.	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells.	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells.	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells.	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells.	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells.	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells.	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells.	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells.	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells.	29435139
fibroblast cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells.	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells.	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells.	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells.	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells.	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells.	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells).	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells.	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells.	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells.	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells.	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells.	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells.	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells.	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells.	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells.	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells.	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells.	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells.	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells.	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells.	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells.	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells.	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells.	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells.	29435139
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生物活性

製品説明

Targets

HDAC1 ^[2] (Cell-free assay)	HDAC3 ^[2] (Cell-free assay)
0.51 μM	1.7 μM

In Vitro
In vitro	MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21^WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. ^[1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. ^[2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. ^[3]
Kinase Assay	Standard HDAC Assays
Kinase Assay	Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λ_ex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. K_m and V_max values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.
細胞実験	細胞株	A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells
	濃度	~ 10 μM
	反応時間	3 days
	実験の流れ	Cancer cells (5 × 10³) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO₂-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na₂HPO₄ is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3 Cleaved PARP Caspase 8 DR4 / DR5 TopoIIα / TopoIIβ		24203492
	Immunofluorescence	phalloidin / snail DR4 / DR5 H3K4Me3 / H3K9Me3		29855565
	Growth inhibition assay	Cell proliferation Cell viability		24203492
	ELISA	GCP-2 / MCP-2 / MIF		24241152

In Vivo
In Vivo	MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. ^[1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. ^[4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. ^[5]
動物実験	動物モデル	A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.
	投与量	12.3, 24.5 and 49 mg/kg
	投与経路	Administered orally once daily 5 days per week for 4 weeks

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04708470	Recruiting	Oropharyngeal Cancer\|Neck Cancer\|Human Papillomavirus\|HPV\|Anal Cancer\|Cervical Cancer\|Penile Cancer\|Vulvar Cancer\|Vaginal Cancer\|Colon Cancer	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	October 5 2021	Phase 1\|Phase 2
NCT03829930	Terminated	Prostate Adenocarcinoma	George Washington University	May 1 2019	Phase 1
NCT03765229	Completed	Melanoma	UNC Lineberger Comprehensive Cancer Center\|Syndax Pharmaceuticals	March 22 2019	Phase 2
NCT03473639	Completed	Metastatic Breast Cancer\|Breast Cancer	University of Virginia\|Syndax Pharmaceuticals	January 29 2019	Phase 1

参考
[1] Saito A, et al. Proc Natl Acad Sci U S A, 1999, 96(8), 4592-4597. [2] Sugawara T, et al. 95th AACR, Orlando, 2004, Abst#2451 [3] Rosato RR, et al. Cancer Res, 2003, 63(13), 3637-3645. [4] Zhang ZY, et al. Neurosci, 2010, 169, 370-377. [5] Kato Y, Clin Cancer Res, 2007, 13(15), 4538-4546. [6] Wegener D, et al. Chem Biol, 2003, 10(1), 61-68. + 展開

参考

+ 展開

化学情報

分子量	376.41	化学式	C₂₁H₂₀N₄O₃
CAS No.	209783-80-2	SDF	Download Entinostat (MS-275) SDFをダウンロードする
Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 75 mg/mL ( (199.25 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問（FAQ）

質問1:
I would like to use Entinostat（Catalog No.S1053） for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?

回答
2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):