Palbociclib Isethionate

別名：PD0332991 Isethionate

製品コード：S1579 純度：99.99%

Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

CAS No. 827022-33-3

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
200mg	JPY 118500	国内在庫あり
1g	JPY 250500	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（278）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Palbociclib Isethionate関連製品

関連ターゲット	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

CDKシグナル伝達経路

CDK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
U-CH6	Growth Inhibition Assay	0-1 μM	72 h	IC50=90 nM	26183925
U-CH3	Growth Inhibition Assay	0-1 μM	72 h	IC50=52 nM	26183925
U-CH2	Growth Inhibition Assay	0-1 μM	72 h	IC50=50.2 nM	26183925
IMR-32	Fuction Assay	0-1 μM	24 h	reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner	26225123
NGP	Fuction Assay	0-1 μM	24 h	reduces the expression of TOP2A, CCNE2, and TK1 in a dose-dependent manner	26225123
SH-EP	Growth Inhibition Assay	1 μM	24 h	induces G1 arrest	26225123
NGP	Growth Inhibition Assay	1 μM	24 h	induces G1 arrest	26225123
SH-SY5Y	Growth Inhibition Assay	1 μM	24 h	induces G1 arrest	26225123
IMR-32	Growth Inhibition Assay	1 μM	24 h	induces G1 arrest	26225123
H596	Growth Inhibition Assay	0-100 μM	72 h	IC50=12 μM	26390342
H520	Growth Inhibition Assay	0-100 μM	72 h	IC50=0.73 μM	26390342
H2170	Growth Inhibition Assay	0-100 μM	72 h	IC50=5 μM	26390342
H157	Growth Inhibition Assay	0-100 μM	72 h	IC50=9 μM	26390342
U-CH7	Growth Inhibition Assay	0-1 μM	72 h	IC50=98 nM	26183925
U-CH11	Growth Inhibition Assay	0-1 μM	72 h	IC50=340 nM	26183925
MCF7	Fuction Assay	2.5-250 nM	24 h	reduces Rb phosphorylation	25991817
MV4-11	Apoptosis Assay	0.5 μM	24 h	enhances apoptosis induced by sorafenib and AC220	25487917
MOLM13	Apoptosis Assay	0.5 μM	24 h	enhances apoptosis induced by sorafenib and AC220	25487917
MCF7	Antitumor assay	100 mg/kg/day	14 days	Antitumor activity against human estrogen-independent human MCF7 cells xenografted in RNU rat assessed as tumor growth inhibition at 100 mg/kg/day, ig administered for 14 days measured on day 15	27448913
MDA-MB-231	Cell cycle arrest assay	0.5 to 1 uM	24 hrs	Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis	24417566
MCF7	Cell cycle arrest assay	0.5 to 1 uM	24 hrs	Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 0.5 to 1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis	24417566
MDA-MB-231	Function assay	0.5 to 5 uM	24 hrs	Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis	24417566
MDA-MB-231	Function assay	0.5 to 5 uM	24 hrs	Inhibition of recombinant CDK4/cyclinD1 in human MDA-MB-231 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis	24417566
MCF7	Function assay	0.5 to 5 uM	24 hrs	Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis	24417566
MCF7	Function assay	0.5 to 5 uM	24 hrs	Inhibition of recombinant CDK4/cyclinD1 in human MCF7 cells assessed as inhibition of retinoblastoma phosphorylation at Ser780 at 0.5 to 5 uM after 24 hrs by Western blotting analysis	24417566
SH-EP	Growth Inhibition Assay		48 h	IC50=2.211 μM	26225123
NGP	Growth Inhibition Assay		48 h	IC50=2.077 μM	26225123
SH-SY5Y	Growth Inhibition Assay		48 h	IC50=676 nM	26225123
IMR-32	Growth Inhibition Assay		48 h	IC50=261 nM	26225123
MOLM13	Function assay		24 hrs	Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs, IC50 = 0.011 μM.	24641103
COLO205	Antiproliferative assay		72 hrs	Antiproliferative activity against Rb-positive human COLO205 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.036 μM.	24641103
MOLM13	Antiproliferative assay		72 hrs	Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM.	24641103
MOLM13	Antiproliferative assay		72 hrs	Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.096 μM.	24641103
U937	Antiproliferative assay		72 hrs	Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis, IC50 = 0.14 μM.	24641103
insect cell	Function assay		2 mins	Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM.	26115571
insect cell	Function assay		2 mins	Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.009 μM.	26115571
insect cell	Function assay		2 mins	Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM.	26115571
insect cell	Function assay		2 mins	Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis, IC50 = 0.011 μM.	26115571
MDA-MB-435	Antiproliferative assay		24 hrs	Antiproliferative activity against Rb-positive human MDA-MB-435 cells assessed as inhibition of [14C]-thymidine incorporation into DNA preincubated for 24 hrs followed by [14C]-thymidine addition measured after 72 hrs by beta plate counting analysis, IC50 = 0.16 μM.	26115571
insect cell	Function assay		2 mins	Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM.	27171036
insect cell	Function assay		2 mins	Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.011 μM.	27171036
insect cell	Function assay		2 mins	Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM.	27171036
insect cell	Function assay		2 mins	Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method, IC50 = 0.015 μM.	27171036
MDA-MB-453	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.137 μM.	27448913
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.24 μM.	27448913
MDA-MB-231	Cytotoxicity assay		48 hrs	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay, IC50 = 0.58 μM.	27448913
A2780	Growth inhibition assay		72 hrs	Growth inhibition of human A2780 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.032 μM.	28156111
MV4-11	Growth inhibition assay		72 hrs	Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50 = 0.05 μM.	28156111
MOLM13	Growth inhibition assay		72 hrs	Growth inhibition of human MOLM13 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.062 μM.	28156111
NB4	Growth inhibition assay		72 hrs	Growth inhibition of human NB4 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.066 μM.	28156111
PC3	Growth inhibition assay		72 hrs	Growth inhibition of human PC3 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.071 μM.	28156111
MDA-MB-453	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-453 cells after 72 hrs by MTT assay, GI50 = 0.326 μM.	28156111
MCF7	Growth inhibition assay		72 hrs	Growth inhibition of human MCF7 cells after 72 hrs by resazurin or MTT assay, GI50 = 0.557 μM.	28156111
M229	Growth inhibition assay		72 hrs	Growth inhibition of human M229 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.22 μM.	28156111
M238	Growth inhibition assay		72 hrs	Growth inhibition of human M238 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.97 μM.	28156111
M249	Growth inhibition assay		72 hrs	Growth inhibition of human M249 cells after 72 hrs by resazurin or MTT assay, GI50 = 1.99 μM.	28156111
M249R	Growth inhibition assay		72 hrs	Growth inhibition of human M249R cells after 72 hrs by resazurin or MTT assay, GI50 = 2.96 μM.	28156111
C4-2B	Growth inhibition assay		72 hrs	Growth inhibition of human C4-2B cells after 72 hrs by resazurin or MTT assay, GI50 = 4.15 μM.	28156111
DU145	Growth inhibition assay		72 hrs	Growth inhibition of human DU145 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.792 μM.	28156111
MDA-MB-468	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-468 cells after 72 hrs by resazurin or MTT assay, GI50 = 5.96 μM.	28156111
BPH1	Growth inhibition assay		72 hrs	Growth inhibition of nontransformed human BPH1 cells after 72 hrs by resazurin or MTT assay, GI50 = 7.442 μM.	28156111
K562	Cytotoxicity assay		96 hrs	Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 2 μM.	24417566
DU145	Cytotoxicity assay		96 hrs	Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay, IC50 = 7.5 μM.	24417566
MV4-11	Function assay		12 to 24 hrs	Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis	28156111
MV4-11	Function assay		12 to 24 hrs	Inhibition of CDK4/6 in human MV4-11 cells assessed as reduction in Rb phosphorylation at Ser780 at GI50 after 12 to 24 hrs by Western blot analysis	28156111
MOLM13-ITD alone	Growth Inhibition Assay			IC50=0.089 ± 0.009 μM	25487917
MV4-11-ITD alone	Growth Inhibition Assay			IC50=0.092 ± 0.008 μM	25487917
MOLM13-ITD/D835Y	Growth Inhibition Assay			IC50=0.114 ± 0.011 μM	25487917
MV4-11-ITD/D835V	Growth Inhibition Assay			IC50=0.116 ± 0.011 μM	25487917
MV4-11-ITD/D835V	Growth Inhibition Assay			IC50=0.102 ± 0.006 μM	25487917
MV4-11-ITD/F691L	Growth Inhibition Assay			IC50=0.112 ± 0.015 μM	25487917
MV4-11-ITD/N841K	Growth Inhibition Assay			IC50=0.113 ± 0.002 μM	25487917
U937-FLT3 WT	Growth Inhibition Assay			IC50=0.102 ± 0.013 μM	25487917
P12-ICHIKAWA	Growth Inhibition assay			IC50 = 0.09604 μM	SANGER
697	Growth Inhibition assay			IC50 = 0.14838 μM	SANGER
NB69	Growth Inhibition assay			IC50 = 0.1618 μM	SANGER
EoL-1-cell	Growth Inhibition assay			IC50 = 0.18726 μM	SANGER
BHT-101	Growth Inhibition assay			IC50 = 0.19825 μM	SANGER
SK-NEP-1	Growth Inhibition assay			IC50 = 0.22002 μM	SANGER
MHH-NB-11	Growth Inhibition assay			IC50 = 0.22019 μM	SANGER
AsPC-1	Growth Inhibition assay			IC50 = 0.25253 μM	SANGER
ES1	Growth Inhibition assay			IC50 = 0.25625 μM	SANGER
LAMA-84	Growth Inhibition assay			IC50 = 0.25819 μM	SANGER
MOLT-16	Growth Inhibition assay			IC50 = 0.25849 μM	SANGER
ES7	Growth Inhibition assay			IC50 = 0.27309 μM	SANGER
KY821	Growth Inhibition assay			IC50 = 0.3141 μM	SANGER
RT-112	Growth Inhibition assay			IC50 = 0.32105 μM	SANGER
HL-60	Growth Inhibition assay			IC50 = 0.34066 μM	SANGER
MOLT-4	Growth Inhibition assay			IC50 = 0.34513 μM	SANGER
KARPAS-45	Growth Inhibition assay			IC50 = 0.37616 μM	SANGER
SK-N-AS	Growth Inhibition assay			IC50 = 0.38783 μM	SANGER
CTB-1	Growth Inhibition assay			IC50 = 0.40502 μM	SANGER
NKM-1	Growth Inhibition assay			IC50 = 0.41189 μM	SANGER
HTC-C3	Growth Inhibition assay			IC50 = 0.43295 μM	SANGER
BE-13	Growth Inhibition assay			IC50 = 0.44427 μM	SANGER
KOSC-2	Growth Inhibition assay			IC50 = 0.4669 μM	SANGER
NB14	Growth Inhibition assay			IC50 = 0.48358 μM	SANGER
CAL-27	Growth Inhibition assay			IC50 = 0.49459 μM	SANGER
H9	Growth Inhibition assay			IC50 = 0.49543 μM	SANGER
RS4-11	Growth Inhibition assay			IC50 = 0.50473 μM	SANGER
PA-1	Growth Inhibition assay			IC50 = 0.50986 μM	SANGER
MV-4-11	Growth Inhibition assay			IC50 = 0.51385 μM	SANGER
OS-RC-2	Growth Inhibition assay			IC50 = 0.52162 μM	SANGER
RPMI-8226	Growth Inhibition assay			IC50 = 0.52686 μM	SANGER
HGC-27	Growth Inhibition assay			IC50 = 0.56499 μM	SANGER
CHP-212	Growth Inhibition assay			IC50 = 0.59359 μM	SANGER
NB10	Growth Inhibition assay			IC50 = 0.59918 μM	SANGER
HH	Growth Inhibition assay			IC50 = 0.59943 μM	SANGER
EW-16	Growth Inhibition assay			IC50 = 0.60352 μM	SANGER
ES8	Growth Inhibition assay			IC50 = 0.60521 μM	SANGER
HAL-01	Growth Inhibition assay			IC50 = 0.60567 μM	SANGER
A204	Growth Inhibition assay			IC50 = 0.63391 μM	SANGER
MHH-PREB-1	Growth Inhibition assay			IC50 = 0.63699 μM	SANGER
EM-2	Growth Inhibition assay			IC50 = 0.65064 μM	SANGER
BV-173	Growth Inhibition assay			IC50 = 0.65248 μM	SANGER
ONS-76	Growth Inhibition assay			IC50 = 0.67782 μM	SANGER
KM-H2	Growth Inhibition assay			IC50 = 0.69554 μM	SANGER
D-263MG	Growth Inhibition assay			IC50 = 0.71712 μM	SANGER
ES3	Growth Inhibition assay			IC50 = 0.72893 μM	SANGER
VA-ES-BJ	Growth Inhibition assay			IC50 = 0.73227 μM	SANGER
NBsusSR	Growth Inhibition assay			IC50 = 0.74299 μM	SANGER
NCI-H520	Growth Inhibition assay			IC50 = 0.74652 μM	SANGER
ES5	Growth Inhibition assay			IC50 = 0.7528 μM	SANGER
T-24	Growth Inhibition assay			IC50 = 0.77871 μM	SANGER
SW962	Growth Inhibition assay			IC50 = 0.80863 μM	SANGER
EW-3	Growth Inhibition assay			IC50 = 0.80876 μM	SANGER
RXF393	Growth Inhibition assay			IC50 = 0.81279 μM	SANGER
U251	Growth Inhibition assay			IC50 = 0.81388 μM	SANGER
CAMA-1	Growth Inhibition assay			IC50 = 0.83394 μM	SANGER
JVM-3	Growth Inhibition assay			IC50 = 0.85178 μM	SANGER
COLO-800	Growth Inhibition assay			IC50 = 0.89778 μM	SANGER
OVCAR-5	Growth Inhibition assay			IC50 = 0.9001 μM	SANGER
LB1047-RCC	Growth Inhibition assay			IC50 = 0.92756 μM	SANGER
SW954	Growth Inhibition assay			IC50 = 0.92941 μM	SANGER
J-RT3-T3-5	Growth Inhibition assay			IC50 = 0.93606 μM	SANGER
Mewo	Growth Inhibition assay			IC50 = 0.9366 μM	SANGER
NCI-H1770	Growth Inhibition assay			IC50 = 0.94055 μM	SANGER
HO-1-N-1	Growth Inhibition assay			IC50 = 0.96281 μM	SANGER
HSC-3	Growth Inhibition assay			IC50 = 0.96648 μM	SANGER
TYK-nu	Growth Inhibition assay			IC50 = 0.99825 μM	SANGER
KYSE-150	Growth Inhibition assay			IC50 = 1.00076 μM	SANGER
SN12C	Growth Inhibition assay			IC50 = 1.00875 μM	SANGER
MOLT-13	Growth Inhibition assay			IC50 = 1.01421 μM	SANGER
TE-11	Growth Inhibition assay			IC50 = 1.04812 μM	SANGER
DB	Growth Inhibition assay			IC50 = 1.07273 μM	SANGER
CAL-39	Growth Inhibition assay			IC50 = 1.07522 μM	SANGER
A3-KAW	Growth Inhibition assay			IC50 = 1.08408 μM	SANGER
CHP-134	Growth Inhibition assay			IC50 = 1.11807 μM	SANGER
TGW	Growth Inhibition assay			IC50 = 1.12395 μM	SANGER
QIMR-WIL	Growth Inhibition assay			IC50 = 1.13134 μM	SANGER
NCI-SNU-1	Growth Inhibition assay			IC50 = 1.16354 μM	SANGER
CGTH-W-1	Growth Inhibition assay			IC50 = 1.17186 μM	SANGER
MHH-ES-1	Growth Inhibition assay			IC50 = 1.17986 μM	SANGER
LB2241-RCC	Growth Inhibition assay			IC50 = 1.1862 μM	SANGER
ML-2	Growth Inhibition assay			IC50 = 1.20734 μM	SANGER
COR-L23	Growth Inhibition assay			IC50 = 1.22933 μM	SANGER
BFTC-905	Growth Inhibition assay			IC50 = 1.24267 μM	SANGER
Hs-578-T	Growth Inhibition assay			IC50 = 1.25817 μM	SANGER
KG-1	Growth Inhibition assay			IC50 = 1.26686 μM	SANGER
HEL	Growth Inhibition assay			IC50 = 1.29338 μM	SANGER
A549	Growth Inhibition assay			IC50 = 1.29399 μM	SANGER
COLO-741	Growth Inhibition assay			IC50 = 1.32089 μM	SANGER
PC-3	Growth Inhibition assay			IC50 = 1.35221 μM	SANGER
HOS	Growth Inhibition assay			IC50 = 1.35296 μM	SANGER
HT-1080	Growth Inhibition assay			IC50 = 1.37519 μM	SANGER
TE-8	Growth Inhibition assay			IC50 = 1.41774 μM	SANGER
BHY	Growth Inhibition assay			IC50 = 1.46923 μM	SANGER
BB65-RCC	Growth Inhibition assay			IC50 = 1.50528 μM	SANGER
HN	Growth Inhibition assay			IC50 = 1.54071 μM	SANGER
NCI-H441	Growth Inhibition assay			IC50 = 1.54907 μM	SANGER
RPMI-8866	Growth Inhibition assay			IC50 = 1.58507 μM	SANGER
CAL-62	Growth Inhibition assay			IC50 = 1.60862 μM	SANGER
MG-63	Growth Inhibition assay			IC50 = 1.61813 μM	SANGER
SK-LU-1	Growth Inhibition assay			IC50 = 1.62152 μM	SANGER
BCPAP	Growth Inhibition assay			IC50 = 1.66457 μM	SANGER
22RV1	Growth Inhibition assay			IC50 = 1.67843 μM	SANGER
T47D	Growth Inhibition assay			IC50 = 1.68061 μM	SANGER
MSTO-211H	Growth Inhibition assay			IC50 = 1.69603 μM	SANGER
DEL	Growth Inhibition assay			IC50 = 1.70273 μM	SANGER
H4	Growth Inhibition assay			IC50 = 1.73212 μM	SANGER
CAL-51	Growth Inhibition assay			IC50 = 1.74855 μM	SANGER
ABC-1	Growth Inhibition assay			IC50 = 1.78582 μM	SANGER
MZ2-MEL	Growth Inhibition assay			IC50 = 1.79542 μM	SANGER
YKG-1	Growth Inhibition assay			IC50 = 1.81061 μM	SANGER
KM12	Growth Inhibition assay			IC50 = 1.81602 μM	SANGER
L-363	Growth Inhibition assay			IC50 = 1.87412 μM	SANGER
KU812	Growth Inhibition assay			IC50 = 1.89282 μM	SANGER
LOXIMVI	Growth Inhibition assay			IC50 = 1.91228 μM	SANGER
G-401	Growth Inhibition assay			IC50 = 1.92428 μM	SANGER
SW780	Growth Inhibition assay			IC50 = 1.96246 μM	SANGER
SW872	Growth Inhibition assay			IC50 = 1.9833 μM	SANGER
NB7	Growth Inhibition assay			IC50 = 1.99323 μM	SANGER
T98G	Growth Inhibition assay			IC50 = 2.00666 μM	SANGER
SW1710	Growth Inhibition assay			IC50 = 2.06945 μM	SANGER
NCI-H1573	Growth Inhibition assay			IC50 = 2.07298 μM	SANGER
KE-37	Growth Inhibition assay			IC50 = 2.08951 μM	SANGER
786-0	Growth Inhibition assay			IC50 = 2.15439 μM	SANGER
SAS	Growth Inhibition assay			IC50 = 2.20374 μM	SANGER
CAL-54	Growth Inhibition assay			IC50 = 2.20413 μM	SANGER
SF268	Growth Inhibition assay			IC50 = 2.23122 μM	SANGER
SW620	Growth Inhibition assay			IC50 = 2.26169 μM	SANGER
MN-60	Growth Inhibition assay			IC50 = 2.3106 μM	SANGER
EFO-27	Growth Inhibition assay			IC50 = 2.32058 μM	SANGER
NCI-H747	Growth Inhibition assay			IC50 = 2.32199 μM	SANGER
HCC2218	Growth Inhibition assay			IC50 = 2.35374 μM	SANGER
MIA-PaCa-2	Growth Inhibition assay			IC50 = 2.36437 μM	SANGER
SJSA-1	Growth Inhibition assay			IC50 = 2.37796 μM	SANGER
RKO	Growth Inhibition assay			IC50 = 2.38496 μM	SANGER
NB6	Growth Inhibition assay			IC50 = 2.40374 μM	SANGER
ES4	Growth Inhibition assay			IC50 = 2.45422 μM	SANGER
EGI-1	Growth Inhibition assay			IC50 = 2.46883 μM	SANGER
CTV-1	Growth Inhibition assay			IC50 = 2.52773 μM	SANGER
NCI-H1355	Growth Inhibition assay			IC50 = 2.55951 μM	SANGER
GT3TKB	Growth Inhibition assay			IC50 = 2.59199 μM	SANGER
SK-HEP-1	Growth Inhibition assay			IC50 = 2.59266 μM	SANGER
GAMG	Growth Inhibition assay			IC50 = 2.59394 μM	SANGER
SK-MES-1	Growth Inhibition assay			IC50 = 2.61803 μM	SANGER
RO82-W-1	Growth Inhibition assay			IC50 = 2.62057 μM	SANGER
ECC10	Growth Inhibition assay			IC50 = 2.70206 μM	SANGER
MCF7	Growth Inhibition assay			IC50 = 2.71464 μM	SANGER
D-283MED	Growth Inhibition assay			IC50 = 2.7243 μM	SANGER
RPMI-7951	Growth Inhibition assay			IC50 = 2.75694 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition assay			IC50 = 2.77099 μM	SANGER
KGN	Growth Inhibition assay			IC50 = 2.81884 μM	SANGER
NUGC-3	Growth Inhibition assay			IC50 = 2.82505 μM	SANGER
NCI-H292	Growth Inhibition assay			IC50 = 2.85053 μM	SANGER
Becker	Growth Inhibition assay			IC50 = 2.95832 μM	SANGER
NCI-H1299	Growth Inhibition assay			IC50 = 3.05263 μM	SANGER
ETK-1	Growth Inhibition assay			IC50 = 3.0543 μM	SANGER
TK10	Growth Inhibition assay			IC50 = 3.20165 μM	SANGER
VMRC-RCZ	Growth Inhibition assay			IC50 = 3.36488 μM	SANGER
YH-13	Growth Inhibition assay			IC50 = 3.44079 μM	SANGER
DU-145	Growth Inhibition assay			IC50 = 3.46269 μM	SANGER
SW1088	Growth Inhibition assay			IC50 = 3.4747 μM	SANGER
HOP-92	Growth Inhibition assay			IC50 = 3.50342 μM	SANGER
KP-N-YS	Growth Inhibition assay			IC50 = 3.62139 μM	SANGER
NCI-H460	Growth Inhibition assay			IC50 = 3.6673 μM	SANGER
U-2-OS	Growth Inhibition assay			IC50 = 3.72535 μM	SANGER
A101D	Growth Inhibition assay			IC50 = 3.76936 μM	SANGER
MDA-MB-231	Growth Inhibition assay			IC50 = 3.81951 μM	SANGER
IST-MES1	Growth Inhibition assay			IC50 = 3.832 μM	SANGER
COR-L105	Growth Inhibition assay			IC50 = 4.018 μM	SANGER
NCI-H1437	Growth Inhibition assay			IC50 = 4.02302 μM	SANGER
CAL-85-1	Growth Inhibition assay			IC50 = 4.02461 μM	SANGER
MZ1-PC	Growth Inhibition assay			IC50 = 4.18556 μM	SANGER
VM-CUB-1	Growth Inhibition assay			IC50 = 4.31284 μM	SANGER
CHL-1	Growth Inhibition assay			IC50 = 4.32169 μM	SANGER
MDA-MB-361	Growth Inhibition assay			IC50 = 4.33153 μM	SANGER
NCI-H661	Growth Inhibition assay			IC50 = 4.50092 μM	SANGER
EW-11	Growth Inhibition assay			IC50 = 4.52231 μM	SANGER
BEN	Growth Inhibition assay			IC50 = 4.52815 μM	SANGER
BFTC-909	Growth Inhibition assay			IC50 = 4.56275 μM	SANGER
NCI-H2087	Growth Inhibition assay			IC50 = 4.58164 μM	SANGER
RVH-421	Growth Inhibition assay			IC50 = 4.6669 μM	SANGER
P30-OHK	Growth Inhibition assay			IC50 = 4.68008 μM	SANGER
NCI-H28	Growth Inhibition assay			IC50 = 4.81661 μM	SANGER
ES6	Growth Inhibition assay			IC50 = 4.83016 μM	SANGER
769-P	Growth Inhibition assay			IC50 = 4.85926 μM	SANGER
OE33	Growth Inhibition assay			IC50 = 4.88161 μM	SANGER
SW982	Growth Inhibition assay			IC50 = 4.95061 μM	SANGER
A388	Growth Inhibition assay			IC50 = 5.02983 μM	SANGER
TI-73	Growth Inhibition assay			IC50 = 5.06194 μM	SANGER
HCT-116	Growth Inhibition assay			IC50 = 5.09889 μM	SANGER
HuP-T3	Growth Inhibition assay			IC50 = 5.18709 μM	SANGER
G-402	Growth Inhibition assay			IC50 = 5.19416 μM	SANGER
NCI-H1792	Growth Inhibition assay			IC50 = 5.24622 μM	SANGER
NCI-H209	Growth Inhibition assay			IC50 = 5.25942 μM	SANGER
NCI-H1650	Growth Inhibition assay			IC50 = 5.30634 μM	SANGER
LCLC-97TM1	Growth Inhibition assay			IC50 = 5.31808 μM	SANGER
S-117	Growth Inhibition assay			IC50 = 5.36976 μM	SANGER
GI-ME-N	Growth Inhibition assay			IC50 = 5.39681 μM	SANGER
NCI-H2122	Growth Inhibition assay			IC50 = 5.49397 μM	SANGER
NCI-H1793	Growth Inhibition assay			IC50 = 5.67593 μM	SANGER
C2BBe1	Growth Inhibition assay			IC50 = 5.70088 μM	SANGER
TE-12	Growth Inhibition assay			IC50 = 5.80556 μM	SANGER
LCLC-103H	Growth Inhibition assay			IC50 = 5.917 μM	SANGER
A673	Growth Inhibition assay			IC50 = 5.91932 μM	SANGER
BB30-HNC	Growth Inhibition assay			IC50 = 5.9836 μM	SANGER
SF295	Growth Inhibition assay			IC50 = 6.00422 μM	SANGER
KU-19-19	Growth Inhibition assay			IC50 = 6.01731 μM	SANGER
CFPAC-1	Growth Inhibition assay			IC50 = 6.04443 μM	SANGER
LoVo	Growth Inhibition assay			IC50 = 6.05063 μM	SANGER
8505C	Growth Inhibition assay			IC50 = 6.07573 μM	SANGER
GMS-10	Growth Inhibition assay			IC50 = 6.15002 μM	SANGER
Ca9-22	Growth Inhibition assay			IC50 = 6.1671 μM	SANGER
DOK	Growth Inhibition assay			IC50 = 6.22072 μM	SANGER
FADU	Growth Inhibition assay			IC50 = 6.26039 μM	SANGER
BxPC-3	Growth Inhibition assay			IC50 = 6.2732 μM	SANGER
CAL-33	Growth Inhibition assay			IC50 = 6.29201 μM	SANGER
SHP-77	Growth Inhibition assay			IC50 = 6.31512 μM	SANGER
LXF-289	Growth Inhibition assay			IC50 = 6.33455 μM	SANGER
GB-1	Growth Inhibition assay			IC50 = 6.382 μM	SANGER
KS-1	Growth Inhibition assay			IC50 = 6.38447 μM	SANGER
D-502MG	Growth Inhibition assay			IC50 = 6.42376 μM	SANGER
LAN-6	Growth Inhibition assay			IC50 = 6.51023 μM	SANGER
H-EMC-SS	Growth Inhibition assay			IC50 = 6.56147 μM	SANGER
LC-2-ad	Growth Inhibition assay			IC50 = 6.60076 μM	SANGER
NCI-H1693	Growth Inhibition assay			IC50 = 6.62215 μM	SANGER
SK-N-FI	Growth Inhibition assay			IC50 = 6.75044 μM	SANGER
D-423MG	Growth Inhibition assay			IC50 = 6.76117 μM	SANGER
KNS-42	Growth Inhibition assay			IC50 = 6.78197 μM	SANGER
GCT	Growth Inhibition assay			IC50 = 6.938 μM	SANGER
DSH1	Growth Inhibition assay			IC50 = 7.0633 μM	SANGER
D-247MG	Growth Inhibition assay			IC50 = 7.07881 μM	SANGER
NCI-SNU-5	Growth Inhibition assay			IC50 = 7.18371 μM	SANGER
TE-6	Growth Inhibition assay			IC50 = 7.20601 μM	SANGER
NOMO-1	Growth Inhibition assay			IC50 = 7.22127 μM	SANGER
NB17	Growth Inhibition assay			IC50 = 7.30309 μM	SANGER
EW-22	Growth Inhibition assay			IC50 = 7.34348 μM	SANGER
EW-13	Growth Inhibition assay			IC50 = 7.35162 μM	SANGER
DOHH-2	Growth Inhibition assay			IC50 = 7.4402 μM	SANGER
TGBC1TKB	Growth Inhibition assay			IC50 = 7.49899 μM	SANGER
GR-ST	Growth Inhibition assay			IC50 = 7.52594 μM	SANGER
KYSE-520	Growth Inhibition assay			IC50 = 7.55515 μM	SANGER
CAPAN-1	Growth Inhibition assay			IC50 = 7.5951 μM	SANGER
HCE-4	Growth Inhibition assay			IC50 = 7.62279 μM	SANGER
MLMA	Growth Inhibition assay			IC50 = 7.62957 μM	SANGER
HT-144	Growth Inhibition assay			IC50 = 7.65368 μM	SANGER
KYSE-180	Growth Inhibition assay			IC50 = 7.71169 μM	SANGER
TE-5	Growth Inhibition assay			IC50 = 7.95971 μM	SANGER
IGROV-1	Growth Inhibition assay			IC50 = 7.98551 μM	SANGER
NCI-H1581	Growth Inhibition assay			IC50 = 8.012 μM	SANGER
SW1990	Growth Inhibition assay			IC50 = 8.04659 μM	SANGER
EFM-19	Growth Inhibition assay			IC50 = 8.08545 μM	SANGER
IGR-1	Growth Inhibition assay			IC50 = 8.43023 μM	SANGER
U-118-MG	Growth Inhibition assay			IC50 = 8.43463 μM	SANGER
SK-OV-3	Growth Inhibition assay			IC50 = 8.46765 μM	SANGER
KNS-62	Growth Inhibition assay			IC50 = 8.51761 μM	SANGER
GOTO	Growth Inhibition assay			IC50 = 8.57635 μM	SANGER
8305C	Growth Inhibition assay			IC50 = 8.70484 μM	SANGER
RPMI-2650	Growth Inhibition assay			IC50 = 8.71955 μM	SANGER
NEC8	Growth Inhibition assay			IC50 = 8.74307 μM	SANGER
KYSE-450	Growth Inhibition assay			IC50 = 8.86548 μM	SANGER
RMG-I	Growth Inhibition assay			IC50 = 9.14058 μM	SANGER
CAKI-1	Growth Inhibition assay			IC50 = 9.31979 μM	SANGER
KYSE-510	Growth Inhibition assay			IC50 = 9.35778 μM	SANGER
A4-Fuk	Growth Inhibition assay			IC50 = 9.36701 μM	SANGER
AN3-CA	Growth Inhibition assay			IC50 = 9.45444 μM	SANGER
SK-N-DZ	Growth Inhibition assay			IC50 = 9.72849 μM	SANGER
HSC-2	Growth Inhibition assay			IC50 = 9.76629 μM	SANGER
EW-1	Growth Inhibition assay			IC50 = 9.79369 μM	SANGER
D-566MG	Growth Inhibition assay			IC50 = 9.83664 μM	SANGER
COLO-792	Growth Inhibition assay			IC50 = 9.98746 μM	SANGER
TE-10	Growth Inhibition assay			IC50 = 10.0396 μM	SANGER
NCI-H650	Growth Inhibition assay			IC50 = 10.4286 μM	SANGER
U-266	Growth Inhibition assay			IC50 = 10.455 μM	SANGER
Detroit562	Growth Inhibition assay			IC50 = 11.0515 μM	SANGER
NH-12	Growth Inhibition assay			IC50 = 11.1446 μM	SANGER
OC-314	Growth Inhibition assay			IC50 = 11.2842 μM	SANGER
IST-MEL1	Growth Inhibition assay			IC50 = 11.5323 μM	SANGER
KNS-81-FD	Growth Inhibition assay			IC50 = 11.5527 μM	SANGER
SW1463	Growth Inhibition assay			IC50 = 11.5989 μM	SANGER
NCI-H23	Growth Inhibition assay			IC50 = 11.6553 μM	SANGER
SK-MEL-2	Growth Inhibition assay			IC50 = 11.7197 μM	SANGER
NB13	Growth Inhibition assay			IC50 = 12.1495 μM	SANGER
Daoy	Growth Inhibition assay			IC50 = 12.2855 μM	SANGER
NCI-H1623	Growth Inhibition assay			IC50 = 12.3801 μM	SANGER
NMC-G1	Growth Inhibition assay			IC50 = 12.717 μM	SANGER
DK-MG	Growth Inhibition assay			IC50 = 12.9482 μM	SANGER
TCCSUP	Growth Inhibition assay			IC50 = 13.1284 μM	SANGER
SCC-15	Growth Inhibition assay			IC50 = 13.2651 μM	SANGER
NOS-1	Growth Inhibition assay			IC50 = 13.2893 μM	SANGER
RH-1	Growth Inhibition assay			IC50 = 13.3037 μM	SANGER
SK-MEL-3	Growth Inhibition assay			IC50 = 13.3728 μM	SANGER
NB5	Growth Inhibition assay			IC50 = 13.4067 μM	SANGER
SNU-387	Growth Inhibition assay			IC50 = 13.5072 μM	SANGER
CAL-120	Growth Inhibition assay			IC50 = 13.6718 μM	SANGER
LNCaP-Clone-FGC	Growth Inhibition assay			IC50 = 13.7991 μM	SANGER
ACN	Growth Inhibition assay			IC50 = 14.0288 μM	SANGER
SK-MEL-30	Growth Inhibition assay			IC50 = 14.063 μM	SANGER
COLO-678	Growth Inhibition assay			IC50 = 14.0822 μM	SANGER
SCC-9	Growth Inhibition assay			IC50 = 14.1021 μM	SANGER
KINGS-1	Growth Inhibition assay			IC50 = 14.1402 μM	SANGER
LS-513	Growth Inhibition assay			IC50 = 14.187 μM	SANGER
HLE	Growth Inhibition assay			IC50 = 14.3852 μM	SANGER
SW1573	Growth Inhibition assay			IC50 = 14.4435 μM	SANGER
KYSE-140	Growth Inhibition assay			IC50 = 14.6327 μM	SANGER
SK-PN-DW	Growth Inhibition assay			IC50 = 14.8001 μM	SANGER
A253	Growth Inhibition assay			IC50 = 15.0625 μM	SANGER
CAL-12T	Growth Inhibition assay			IC50 = 15.4662 μM	SANGER
COLO-679	Growth Inhibition assay			IC50 = 15.7683 μM	SANGER
UACC-257	Growth Inhibition assay			IC50 = 16.1201 μM	SANGER
U-87-MG	Growth Inhibition assay			IC50 = 16.3523 μM	SANGER
HCC1806	Growth Inhibition assay			IC50 = 16.7071 μM	SANGER
NCI-H2170	Growth Inhibition assay			IC50 = 17.2448 μM	SANGER
AGS	Growth Inhibition assay			IC50 = 17.3808 μM	SANGER
MEL-HO	Growth Inhibition assay			IC50 = 17.7503 μM	SANGER
SW48	Growth Inhibition assay			IC50 = 17.7716 μM	SANGER
HuP-T4	Growth Inhibition assay			IC50 = 18.0206 μM	SANGER
NCI-H720	Growth Inhibition assay			IC50 = 18.1402 μM	SANGER
RCC10RGB	Growth Inhibition assay			IC50 = 18.1697 μM	SANGER
HD-MY-Z	Growth Inhibition assay			IC50 = 18.2254 μM	SANGER
A427	Growth Inhibition assay			IC50 = 18.5094 μM	SANGER
HCC2998	Growth Inhibition assay			IC50 = 18.6051 μM	SANGER
EPLC-272H	Growth Inhibition assay			IC50 = 19.0434 μM	SANGER
C32	Growth Inhibition assay			IC50 = 19.045 μM	SANGER
UMC-11	Growth Inhibition assay			IC50 = 19.2123 μM	SANGER
CaR-1	Growth Inhibition assay			IC50 = 19.6804 μM	SANGER
KYSE-410	Growth Inhibition assay			IC50 = 19.9139 μM	SANGER
HuCCT1	Growth Inhibition assay			IC50 = 20.6293 μM	SANGER
LB996-RCC	Growth Inhibition assay			IC50 = 20.7168 μM	SANGER
KYSE-70	Growth Inhibition assay			IC50 = 20.8059 μM	SANGER
CAL-72	Growth Inhibition assay			IC50 = 20.915 μM	SANGER
Capan-2	Growth Inhibition assay			IC50 = 21.0413 μM	SANGER
PANC-08-13	Growth Inhibition assay			IC50 = 21.2515 μM	SANGER
SBC-1	Growth Inhibition assay			IC50 = 21.3081 μM	SANGER
MFM-223	Growth Inhibition assay			IC50 = 21.3342 μM	SANGER
BB49-HNC	Growth Inhibition assay			IC50 = 21.5716 μM	SANGER
SH-4	Growth Inhibition assay			IC50 = 21.6618 μM	SANGER
HuO9	Growth Inhibition assay			IC50 = 21.9825 μM	SANGER
AM-38	Growth Inhibition assay			IC50 = 22.0485 μM	SANGER
A431	Growth Inhibition assay			IC50 = 23.2119 μM	SANGER
YAPC	Growth Inhibition assay			IC50 = 23.2651 μM	SANGER
LU-139	Growth Inhibition assay			IC50 = 23.4809 μM	SANGER
HEC-1	Growth Inhibition assay			IC50 = 23.4937 μM	SANGER
SCC-25	Growth Inhibition assay			IC50 = 24.3006 μM	SANGER
HT-29	Growth Inhibition assay			IC50 = 24.3823 μM	SANGER
PC-14	Growth Inhibition assay			IC50 = 24.6571 μM	SANGER
Calu-6	Growth Inhibition assay			IC50 = 25.5071 μM	SANGER
SJRH30	Growth Inhibition assay			IC50 = 25.6496 μM	SANGER
ChaGo-K-1	Growth Inhibition assay			IC50 = 26.1629 μM	SANGER
IA-LM	Growth Inhibition assay			IC50 = 26.3645 μM	SANGER
GP5d	Growth Inhibition assay			IC50 = 26.4491 μM	SANGER
NCI-H2291	Growth Inhibition assay			IC50 = 26.6541 μM	SANGER
BALL-1	Growth Inhibition assay			IC50 = 26.9397 μM	SANGER
HCC1954	Growth Inhibition assay			IC50 = 26.9808 μM	SANGER
NCI-H2452	Growth Inhibition assay			IC50 = 27.4163 μM	SANGER
LU-99A	Growth Inhibition assay			IC50 = 27.5582 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition assay			IC50 = 27.7299 μM	SANGER
PANC-10-05	Growth Inhibition assay			IC50 = 27.7775 μM	SANGER
NCI-H2405	Growth Inhibition assay			IC50 = 27.9387 μM	SANGER
MDA-MB-415	Growth Inhibition assay			IC50 = 28.4137 μM	SANGER
NCI-H2342	Growth Inhibition assay			IC50 = 28.5281 μM	SANGER
TGBC24TKB	Growth Inhibition assay			IC50 = 28.7117 μM	SANGER
LU-134-A	Growth Inhibition assay			IC50 = 28.9261 μM	SANGER
SCC-4	Growth Inhibition assay			IC50 = 31.0495 μM	SANGER
Saos-2	Growth Inhibition assay			IC50 = 31.9306 μM	SANGER
RERF-LC-MS	Growth Inhibition assay			IC50 = 32.8231 μM	SANGER
M14	Growth Inhibition assay			IC50 = 32.9764 μM	SANGER
HPAF-II	Growth Inhibition assay			IC50 = 33.5011 μM	SANGER
NCI-H1755	Growth Inhibition assay			IC50 = 34.3305 μM	SANGER
D-392MG	Growth Inhibition assay			IC50 = 35.8674 μM	SANGER
A704	Growth Inhibition assay			IC50 = 36.0427 μM	SANGER
CP50-MEL-B	Growth Inhibition assay			IC50 = 36.1911 μM	SANGER
EW-18	Growth Inhibition assay			IC50 = 36.452 μM	SANGER
WM-115	Growth Inhibition assay			IC50 = 36.8099 μM	SANGER
LU-65	Growth Inhibition assay			IC50 = 37.1417 μM	SANGER
NCI-H1563	Growth Inhibition assay			IC50 = 37.2484 μM	SANGER
DBTRG-05MG	Growth Inhibition assay			IC50 = 38.0691 μM	SANGER
NCI-H630	Growth Inhibition assay			IC50 = 38.4714 μM	SANGER
NCI-H1155	Growth Inhibition assay			IC50 = 39.242 μM	SANGER
OVCAR-3	Growth Inhibition assay			IC50 = 39.9195 μM	SANGER
OAW-42	Growth Inhibition assay			IC50 = 40.4258 μM	SANGER
JVM-2	Growth Inhibition assay			IC50 = 41.2415 μM	SANGER
C3A	Growth Inhibition assay			IC50 = 41.3447 μM	SANGER
HT55	Growth Inhibition assay			IC50 = 42.2841 μM	SANGER
OVCAR-4	Growth Inhibition assay			IC50 = 42.2974 μM	SANGER
MEG-01	Growth Inhibition assay			IC50 = 42.4616 μM	SANGER
NCI-H82	Growth Inhibition assay			IC50 = 43.9892 μM	SANGER
JEG-3	Growth Inhibition assay			IC50 = 44.947 μM	SANGER
BPH-1	Growth Inhibition assay			IC50 = 46.3998 μM	SANGER
MPP-89	Growth Inhibition assay			IC50 = 47.2898 μM	SANGER
ALL-PO	Growth Inhibition assay			IC50 = 47.4188 μM	SANGER
HT	Growth Inhibition assay			IC50 = 47.492 μM	SANGER
NCI-H2347	Growth Inhibition assay			IC50 = 48.0715 μM	SANGER
A2780	Growth Inhibition assay			IC50 = 49.4228 μM	SANGER
KARPAS-299	Growth Inhibition assay			IC50 = 49.5119 μM	SANGER
NCI-H1651	Growth Inhibition assay			IC50 = 49.8821 μM	SANGER
OCI-AML2	Growth Inhibition assay			IC50 = 50.2084 μM	SANGER
OCUB-M	Growth Inhibition assay			IC50 = 50.3047 μM	SANGER
HuH-7	Growth Inhibition assay			IC50 = 50.5943 μM	SANGER
RCM-1	Growth Inhibition assay			IC50 = 50.9133 μM	SANGER
FTC-133	Growth Inhibition assay			IC50 = 51.322 μM	SANGER
PSN1	Growth Inhibition assay			IC50 = 51.4335 μM	SANGER
A498	Growth Inhibition assay			IC50 = 52.0995 μM	SANGER
SF126	Growth Inhibition assay			IC50 = 52.6568 μM	SANGER
UACC-62	Growth Inhibition assay			IC50 = 55.2224 μM	SANGER
PANC-03-27	Growth Inhibition assay			IC50 = 56.6788 μM	SANGER
NCI-H727	Growth Inhibition assay			IC50 = 56.8127 μM	SANGER
SNU-423	Growth Inhibition assay			IC50 = 57.2859 μM	SANGER
LB771-HNC	Growth Inhibition assay			IC50 = 57.8405 μM	SANGER
HCC1395	Growth Inhibition assay			IC50 = 58.0464 μM	SANGER
OAW-28	Growth Inhibition assay			IC50 = 58.2785 μM	SANGER
NB12	Growth Inhibition assay			IC50 = 60.6696 μM	SANGER
DJM-1	Growth Inhibition assay			IC50 = 60.7331 μM	SANGER
MDA-MB-157	Growth Inhibition assay			IC50 = 61.1649 μM	SANGER
DU-4475	Growth Inhibition assay			IC50 = 62.5495 μM	SANGER
RD	Growth Inhibition assay			IC50 = 62.7387 μM	SANGER
LS-123	Growth Inhibition assay			IC50 = 63.2618 μM	SANGER
NCI-H226	Growth Inhibition assay			IC50 = 64.22 μM	SANGER
MS-1	Growth Inhibition assay			IC50 = 64.8358 μM	SANGER
no-10	Growth Inhibition assay			IC50 = 65.7473 μM	SANGER
SW626	Growth Inhibition assay			IC50 = 65.7579 μM	SANGER
DMS-273	Growth Inhibition assay			IC50 = 66.2296 μM	SANGER
ESS-1	Growth Inhibition assay			IC50 = 66.5096 μM	SANGER
TE-9	Growth Inhibition assay			IC50 = 66.6316 μM	SANGER
CAS-1	Growth Inhibition assay			IC50 = 67.7954 μM	SANGER
639-V	Growth Inhibition assay			IC50 = 69.4198 μM	SANGER
GAK	Growth Inhibition assay			IC50 = 70.2031 μM	SANGER
NCI-H526	Growth Inhibition assay			IC50 = 71.0913 μM	SANGER
DoTc2-4510	Growth Inhibition assay			IC50 = 71.443 μM	SANGER
647-V	Growth Inhibition assay			IC50 = 73.2118 μM	SANGER
OVCAR-8	Growth Inhibition assay			IC50 = 73.2367 μM	SANGER
COLO-680N	Growth Inhibition assay			IC50 = 75.2497 μM	SANGER
HDLM-2	Growth Inhibition assay			IC50 = 75.7806 μM	SANGER
TGBC11TKB	Growth Inhibition assay			IC50 = 79.0192 μM	SANGER
DMS-114	Growth Inhibition assay			IC50 = 81.9577 μM	SANGER
CW-2	Growth Inhibition assay			IC50 = 82.6818 μM	SANGER
MDA-MB-175-VII	Growth Inhibition assay			IC50 = 85.3135 μM	SANGER
HT-1376	Growth Inhibition assay			IC50 = 85.846 μM	SANGER
SW1417	Growth Inhibition assay			IC50 = 88.2906 μM	SANGER
HCE-T	Growth Inhibition assay			IC50 = 91.7205 μM	SANGER
OE19	Growth Inhibition assay			IC50 = 92.7944 μM	SANGER
NCI-N87	Growth Inhibition assay			IC50 = 92.8881 μM	SANGER
SNU-449	Growth Inhibition assay			IC50 = 93.584 μM	SANGER
NCI-H1092	Growth Inhibition assay			IC50 = 96.5851 μM	SANGER
COLO-684	Growth Inhibition assay			IC50 = 99.0686 μM	SANGER
HCC1937	Growth Inhibition assay			IC50 = 99.9315 μM	SANGER
EFO-21	Growth Inhibition assay			IC50 = 110.988 μM	SANGER
ZR-75-30	Growth Inhibition assay			IC50 = 114.117 μM	SANGER
HCC1187	Growth Inhibition assay			IC50 = 114.179 μM	SANGER
SW684	Growth Inhibition assay			IC50 = 114.655 μM	SANGER
AU565	Growth Inhibition assay			IC50 = 115.892 μM	SANGER
HCC38	Growth Inhibition assay			IC50 = 116.559 μM	SANGER
LK-2	Growth Inhibition assay			IC50 = 119.652 μM	SANGER
LB2518-MEL	Growth Inhibition assay			IC50 = 122.428 μM	SANGER
COLO-320-HSR	Growth Inhibition assay			IC50 = 126.212 μM	SANGER
HCC1419	Growth Inhibition assay			IC50 = 129.227 μM	SANGER
NCI-H2228	Growth Inhibition assay			IC50 = 129.321 μM	SANGER
NCI-H2052	Growth Inhibition assay			IC50 = 130.358 μM	SANGER
HCC2157	Growth Inhibition assay			IC50 = 133.973 μM	SANGER
HCC1569	Growth Inhibition assay			IC50 = 135.05 μM	SANGER
HuO-3N1	Growth Inhibition assay			IC50 = 135.366 μM	SANGER
MZ7-mel	Growth Inhibition assay			IC50 = 145.604 μM	SANGER
SW756	Growth Inhibition assay			IC50 = 147.143 μM	SANGER
NCI-H1304	Growth Inhibition assay			IC50 = 149.222 μM	SANGER
LN-405	Growth Inhibition assay			IC50 = 149.732 μM	SANGER
BT-474	Growth Inhibition assay			IC50 = 150.969 μM	SANGER
LS-411N	Growth Inhibition assay			IC50 = 152.319 μM	SANGER
ATN-1	Growth Inhibition assay			IC50 = 152.458 μM	SANGER
SNU-C2B	Growth Inhibition assay			IC50 = 153.444 μM	SANGER
KYSE-270	Growth Inhibition assay			IC50 = 155.75 μM	SANGER
NCI-H1395	Growth Inhibition assay			IC50 = 156.493 μM	SANGER
EKVX	Growth Inhibition assay			IC50 = 156.981 μM	SANGER
HCC70	Growth Inhibition assay			IC50 = 157.989 μM	SANGER
NCI-H522	Growth Inhibition assay			IC50 = 161.368 μM	SANGER
Ca-Ski	Growth Inhibition assay			IC50 = 161.86 μM	SANGER
SW1116	Growth Inhibition assay			IC50 = 163.382 μM	SANGER
8-MG-BA	Growth Inhibition assay			IC50 = 165.797 μM	SANGER
NCI-H1048	Growth Inhibition assay			IC50 = 172.374 μM	SANGER
RH-18	Growth Inhibition assay			IC50 = 172.601 μM	SANGER
LU-135	Growth Inhibition assay			IC50 = 173.259 μM	SANGER
SW948	Growth Inhibition assay			IC50 = 174.6 μM	SANGER
LS-1034	Growth Inhibition assay			IC50 = 183.742 μM	SANGER
SCH	Growth Inhibition assay			IC50 = 187.022 μM	SANGER
KP-N-YN	Growth Inhibition assay			IC50 = 192.971 μM	SANGER
NCI-H69	Growth Inhibition assay			IC50 = 210.925 μM	SANGER
SBC-5	Growth Inhibition assay			IC50 = 211.162 μM	SANGER
MFE-280	Growth Inhibition assay			IC50 = 212.067 μM	SANGER
MC116	Growth Inhibition assay			IC50 = 212.736 μM	SANGER
BT-20	Growth Inhibition assay			IC50 = 216.38 μM	SANGER
NCI-H1993	Growth Inhibition assay			IC50 = 217.295 μM	SANGER
Calu-3	Growth Inhibition assay			IC50 = 217.37 μM	SANGER
GCIY	Growth Inhibition assay			IC50 = 221.332 μM	SANGER
HT-3	Growth Inhibition assay			IC50 = 222.173 μM	SANGER
MC-IXC	Growth Inhibition assay			IC50 = 227.215 μM	SANGER
COR-L88	Growth Inhibition assay			IC50 = 234.259 μM	SANGER
SK-MEL-1	Growth Inhibition assay			IC50 = 235.59 μM	SANGER
MDA-MB-453	Growth Inhibition assay			IC50 = 236.33 μM	SANGER
SiHa	Growth Inhibition assay			IC50 = 247.22 μM	SANGER
C8166	Growth Inhibition assay			IC50 = 251.341 μM	SANGER
SKG-IIIa	Growth Inhibition assay			IC50 = 251.504 μM	SANGER
HT-1197	Growth Inhibition assay			IC50 = 268.492 μM	SANGER
no-11	Growth Inhibition assay			IC50 = 291.357 μM	SANGER
ME-180	Growth Inhibition assay			IC50 = 296.912 μM	SANGER
NY	Growth Inhibition assay			IC50 = 320.632 μM	SANGER
C-33-A	Growth Inhibition assay			IC50 = 325.06 μM	SANGER
NCI-H2029	Growth Inhibition assay			IC50 = 338.305 μM	SANGER
IST-SL1	Growth Inhibition assay			IC50 = 342.105 μM	SANGER
KLE	Growth Inhibition assay			IC50 = 347.29 μM	SANGER
SF539	Growth Inhibition assay			IC50 = 348.01 μM	SANGER
5637	Growth Inhibition assay			IC50 = 360.37 μM	SANGER
COLO-824	Growth Inhibition assay			IC50 = 363.58 μM	SANGER
NCI-H810	Growth Inhibition assay			IC50 = 363.938 μM	SANGER
JAR	Growth Inhibition assay			IC50 = 365.01 μM	SANGER
L-428	Growth Inhibition assay			IC50 = 369.277 μM	SANGER
COLO-668	Growth Inhibition assay			IC50 = 387.033 μM	SANGER
GI-1	Growth Inhibition assay			IC50 = 398.59 μM	SANGER
NCI-H446	Growth Inhibition assay			IC50 = 399.497 μM	SANGER
CCRF-CEM	Growth Inhibition assay			IC50 = 403.587 μM	SANGER
T84	Growth Inhibition assay			IC50 = 403.686 μM	SANGER
K-562	Growth Inhibition assay			IC50 = 432.947 μM	SANGER
OMC-1	Growth Inhibition assay			IC50 = 433.814 μM	SANGER
LB831-BLC	Growth Inhibition assay			IC50 = 434.556 μM	SANGER
BT-549	Growth Inhibition assay			IC50 = 435.102 μM	SANGER
MKN7	Growth Inhibition assay			IC50 = 439.822 μM	SANGER
SW1783	Growth Inhibition assay			IC50 = 449.251 μM	SANGER
SNB75	Growth Inhibition assay			IC50 = 486.478 μM	SANGER
M059J	Growth Inhibition assay			IC50 = 492.923 μM	SANGER
KURAMOCHI	Growth Inhibition assay			IC50 = 498.612 μM	SANGER
TE-1	Growth Inhibition assay			IC50 = 502.729 μM	SANGER
NCI-H596	Growth Inhibition assay			IC50 = 530.805 μM	SANGER
PFSK-1	Growth Inhibition assay			IC50 = 532.941 μM	SANGER
sf9	Function assay			Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM.	26851505
sf9	Function assay			Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP, IC50 = 9.2 μM.	26851505
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
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
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
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生物活性

製品説明

Palbociclib Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

特性

The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.

Targets

CDK4/CyclinD3 ^[1] (Cell-free assay)	CDK4/CyclinD1 ^[1] (Cell-free assay)	CDK6/CyclinD2 ^[1] (Cell-free assay)
9 nM	11 nM	15 nM

In Vitro
In vitro	PD 0332991 exhibits absolute selectivity for CDK4/6 with little or no activity against other CDKs. PD 0332991 is effective at reducing Rb phosphorylation at Ser⁷⁸⁰ and Ser⁷⁹⁵ in MDA-MB-435 breast carcinoma cells with IC50 of 66 nM and 63 nM, respectively. PD 0332991 is a potent inhibitor of cell growth and suppresses DNA replication by preventing cells from entering S phase. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast (such as MDA-MB-435, MCF-7), colon (H1299), and lung carcinomas (Colo-205) as well as human leukemias (CRRF-CEM and K562), with IC50 values ranging from 0.04-0.17 μM. PD 0332991 significant increases the percentage of MDA-MB-453 in G1 period. ^[1] PD 0332991 inhibits phosphorylation of Rb in cycling CD138+ primary bone marrow myeloma cells, nontransformed primary B cells, MM1.S and CAG HMCLs cells line with IC50 of <0.1 μM, 0.05 μM, and 60-70 nM, respectively. PD 0332991 treatment also induces G1 arrest of CD138+ primary bone marrow myeloma and nontransformed primary B cells. PD 0332991 induces G1 arrest in MM1.S with IC50 of ~0.05 μM. ^[2] PD 0332991 preferentially inhibits proliferation of luminal estrogen receptor-positive (including HER2-positive) human breast cancer cell lines. PD 0332991 increases gene expression of pRb and cyclin D1 and decreases gene expression of CDKN2A (p16) in most sensitive lines. PD 0332991 enhances sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade. ^[3]
Kinase Assay	CDK activity assays
Kinase Assay	CDK assays for IC50 determinations and kinetic evaluation are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST•RB-Cterm). The total reaction volume is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl₂ 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) containing 0.25 μCi of [γ-³²P]ATP, 20 ng of enzyme, 1 μg of GST•RB-Cterm, and appropriate dilutions of inhibitor. All components except the [γ-³²P]ATP are added to the wells, and placed on a plate mixer for 2 min. The reaction is started by adding the [γ-³²P]ATP, and incubated at 25℃ for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid, and the plate is kept at 4 ℃ for at least 1 hr to allow the substrate to precipitate. The wells are then washed five times with 0.2 mL of 10% trichloroacetic acid, and radioactive incorporation is determined with a β plate counter.
細胞実験	細胞株	Human breast cancer cells MDA-MB-435
	濃度	2 μM
	反応時間	6 days
	実験の流れ	Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of PD 0332991 are added. Control wells without drug are also seeded. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter Z2 particle counter.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	RB1 (pT821) / RB1 (pS780) pAMPKα(T172) / AMPKα pULK1(S317) / ULK1 c-Jun / p-c-Jun / NFκB(p50) p38 / p-P38 / JNK / p-JNK		30300583
	Growth inhibition assay	Cell viability IC50		28453226
	Immunofluorescence	γH2AX(Ser139) LC3B		29669860
	ELISA	PGE2		26540629

In Vivo
In Vivo	PD 0332991(150 mg/kg) produces rapid Colo-205 colon carcinoma xenografts regressions and a corresponding tumor growth delay. PD 0332991 (150 mg/kg) induces complete tumor stasis and cell kill in MDA-MB-435 breast carcinoma. PD 0332991 (150 mg/kg) also induces significant tumor regression in mice bearing the SF-295 glioblastoma xenografts, and in ZR-75-1 breast and PC-3 prostate tumor models (complete suppression of tumor growth). PD 0332991 (150 mg/kg) suppresses Rb Ser⁷⁸⁰ phosphorylation in MDA-MB-435 breast carcinoma over the full 24-hour period. PD 0332991 (150 mg/kg) down-regulates expression of four E2F-regulated genes CDC2, CCNE2, TK1, and TOP2A in Colo-205 carcinoma xenografts. ^[1] PD 0332991 also rapidly inhibits myeloma tumor growth. ^[2]
動物実験	動物モデル	Human colon carcinoma xenografts Colo-205
	投与量	150 mg/kg
	投与経路	o.p. injection every day

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05665361	Recruiting	Advanced Clear Cell Renal Carcinoma (Ccrcc)\|Papillary Renal Cell Carcinoma (Prcc)	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	April 24 2024	Phase 1\|Phase 2
NCT06307457	Completed	Breast Cancer	Pfizer	March 11 2024	--
NCT05709158	Not yet recruiting	Breast Cancer	Pfizer	March 1 2024	--
NCT05912933	Not yet recruiting	Breast Cancer	Pfizer	March 1 2024	--

参考
[1] Fry DW, et al. Mol Cancer Ther, 2004, 3(11), 1427-1438. [2] Baughn LB, et al. Cancer Res, 2006, 66(15), 7661-7667. [3] Finn RS, et al. Breast Cancer Res, 2009, 11(5), R77. [4] Fry DW, et al. J Biol Chem, 2001, 276(20), 16617-16623. + 展開

参考

[4] Fry DW, et al. J Biol Chem, 2001, 276(20), 16617-16623.

+ 展開

化学情報

分子量	573.66	化学式	C₂₄H₂₉N₇O₂.C₂H₆O₄S
CAS No.	827022-33-3	SDF	Download Palbociclib Isethionate SDFをダウンロードする
Smiles	CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.C(CS(=O)(=O)O)O
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:

Water : 100 mg/mL

DMSO : Insoluble ( 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。)

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

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Handling Instructions

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よくある質問（FAQ）

質問1:
What is the best vehicle for palbociclib for in vitro and in vivo?

回答
You can use water for vitro use and Saline for vivo use.

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):