Silmitasertib (CX-4945)

製品コード：S2248 純度：99.98%

Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.

CAS No. 1009820-21-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 43600	国内在庫あり
2mg	JPY 25500	国内在庫あり
5mg	JPY 44500	国内在庫あり
50mg	JPY 133500	国内在庫あり
1g	JPY 595500	国内在庫なし(納期7~10日)

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（137）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Silmitasertib (CX-4945)関連製品

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関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

Casein Kinase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
A549	Function assay	10 uM	4 to 24 hrs	Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method	24012124
A549	Function assay	10 uM	24 hrs	Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method	24012124
A549	Function assay	10 uM		Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method	24012124
A549	Function assay	10 uM	15 to 30 mins	Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method	24012124
A549	Function assay	30 uM	48 hrs	Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography	24012124
Vero E6	Antiviral assay		48 h	IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 3.89045 μM.	32353859
Sf21	Function assay		90 mins	Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50 = 0.003 μM.	29559278
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM.	26850376
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 = 1.8 μM.	24681986
K562	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50 = 7 μM.	23711832
U937	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50 = 4.2 μM.	23711832
MV4-11	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50 = 3 μM.	23711832
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM.	22339433
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM.	22339433
Hs 578T	Antiproliferative assay		4 days	Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50 = 13.1 μM.	21174434
MCF7	Antiproliferative assay		4 days	Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM.	21174434
MDA-MB-231	Antiproliferative assay		4 days	Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50 = 6.4 μM.	21174434
LNCAP	Antiproliferative assay		4 days	Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50 = 4.7 μM.	21174434
BxPC3	Antiproliferative assay		4 days	Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 μM.	21174434
A549	Antiproliferative assay		4 days	Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 3 μM.	21174434
Jurkat	Antiproliferative assay		4 days	Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM.	21174434
HCT116	Antiproliferative assay		4 days	Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 μM.	21174434
MIAPaCa2	Antiproliferative assay		4 days	Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 μM.	21174434
Jurkat	Function assay			Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50 = 0.1 μM.	21174434
HDMEC	Function Assay	1 μM	24 h	affects subcellular localization of NFATc1 and phospho-p65	26381437
HDMEC	Function Assay	0.25/0.5/1 μM	24 h	reduces expression of VCAM-1 but not ICAM-1	26381437
A549	Function Assay	3/10 μM	48 h	suppresses the micropillar-induced expression of p-FAK	26318800
HDMEC	Function Assay	50 μM	1/5 h	decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC	26189586
HDMEC	Kinase Assay	1-50 μM	5 h	decreases CK2 kinase activity without affecting cell viability	26189586
HEK293	Function Assay	3 μM	5 h	CK2 phosphorylates eIF3j at Ser127	25887626
LAMA84	Kinase Assay	0.5 μM	15 min	reduces CK2 kinase activity	25887626
Hela	Kinase Assay	0.5 μM	15 min	reduces CK2 kinase activity	25887626
HEK293	Kinase Assay	0.5 μM	15 min	reduces CK2 kinase activity	25887626
UM-SCC46	Function Assay	0.5/4/10 μM	72 h	down-regulates the expression of NF-ĸB, Bcl-XL, p53, p21, AP-1 and up-regulates the expression IL-8 concentration dependently	25798061
UM-SCC1	Function Assay	0.5/4/10 μM	72 h	down-regulates the expression of NF-ĸB, Bcl-XL and up-regulates the expression of p53, p21, AP-1 and IL-8 concentration dependently	25798061
UM-SCC46	Growth Inhibition Assay	0.1-30 μM	1-5 d	IC50=3.4 μM	25798061
Raji	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
Oci Ly 19	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
Oci Ly 18	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
Oci Ly 1	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
Oci Ly 10	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
Oci Ly 3	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
NU-DUL	Growth Inhibition Assay	5-25 μM	48 h	inhibits cell growth concentration dependently	25788269
H358	Apoptosis Assay	10 μM	72 h	induces apoptosis	25750308
Calu-1	Apoptosis Assay	10 μM	72 h	induces apoptosis	25750308
PC9/ER	Function Assay	5 µM	48 h	induces autophagy	25486409
PC9/GR	Function Assay	5 µM	48 h	induces autophagy	25486409
H2052	Growth Inhibition Assay	0.01-30 μM	72 h	IC50=2.0 μM	25422081
UM-SCC-46	Clonogenic Assay	0.5-5 μM	14 d	inhibits clonogenic survival and sphere formation	25379016
H2170	Function Assay	10 μM	30 min	attenuates PI3K-Akt-mTOR signaling	22387988
A431	Function Assay	10 μM	4-24 h	enhances apoptosis with	22387988
H2170	Function Assay	10 μM	4-24 h	enhances apoptosis with	22387988
LNCap	Growth Inhibition Assay	0-30 μM	4 d	IC50=4.59 μM	22832316
A549	Growth Inhibition Assay	0-30 μM	72 h	IC50=4.15 μM, inhibits cell growth concentration dependently	23651443
H1299	Growth Inhibition Assay	0-30 μM	72 h	IC50=1.80 μM, inhibits cell growth concentration dependently	23651443
A549	Function Assay	1/10 μM	48 h	leads to a dose-dependent decrease in Notch reporter activity	23651443
S-LAMA84	Function Assay	3 μM	24 h	reduces CK2 activity	24012109
A549	Function Assay	10 μM	12/24/48 h	inhibits TGF-β1-induced migration and invasion	24023938
A549	Function Assay	3 μM	48 h	inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist	24023938
U-266	Growth Inhibition Assay	0-40 μM	48 h	IC50=19.8 µM	24086494
Jeko-1	Growth Inhibition Assay	0-40 μM	48 h	IC50=2.4 µM	24086494
INA-6	Growth Inhibition Assay	0-40 μM	48 h	IC50=2.42 µM	24086494
Rec-1	Growth Inhibition Assay	0-40 μM	48 h	IC50=1.46 µM	24086494
CEM-R	Growth Inhibition Assay	1-10 μM	48 h	IC50=4 μM	24253024
Jurkat	Growth Inhibition Assay	1-10 μM	48 h	IC50=4.9 μM	24253024
CEM-S	Growth Inhibition Assay	1-10 μM	48 h	IC50=4.6 μM	24253024
MOLT-4	Growth Inhibition Assay	1-10 μM	48 h	IC50=5.7 μM	24253024
PF-382	Growth Inhibition Assay	1-10 μM	48 h	IC50=4.5 μM	24253024
ALL-SIL	Growth Inhibition Assay	1-10 μM	48 h	IC50=5.7 μM	24253024
DND-41	Growth Inhibition Assay	1-10 μM	48 h	IC50=9 μM	24253024
HPB-ALL	Growth Inhibition Assay	1-10 μM	48 h	IC50=6.1 μM	24253024
ALL-SIL	Apoptosis Assay	5 μM	24/48 h	induces apoptosis	24253024
DND-41	Apoptosis Assay	5 μM	24/48 h	induces apoptosis	24253024
MOLT-4	Apoptosis Assay	5 μM	24/48 h	induces apoptosis	24253024
C2C12	Function Assay	3 μM	12/24/48 h	inhibits the expression of osteoclast differentiation markers and Akt phosphorylation	24293011
Nalm6	Function Assay	10/20 μM	24 h	results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression	24561792
SUP-B15	Function Assay	10/20 μM	24 h	results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression	24561792
SUP-B15	Apoptosis Assay	6/10 μM	48 h	induces apoptosis	24561792
ARPE-19	Kinase Assay	5/10/20 μM	24/48 h	inhibits CK2 kinase activity at a concentration of 5 μM	24686080
ARPE-19	Growth Inhibition Assay	10 μM	24-96 h	inhibits cell growth time dependently	24686080
HCT116	Growth Inhibition Assay	10 μM	24-96 h	inhibits cell growth time dependently	24686080
ARPE-19	Function Assay	10 μM	4 h	causes ER-stress response over the p-eIF2α branch, but does not induce CHOP	24686080
HCT116	Function Assay	10 μM	4 h	causes ER-stress response over the p-eIF2α branch, but does not induce CHOP	24686080
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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
A549	Function assay	1 to 10 uM	24 hrs	Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method	24012124
Jurkat	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50 = 4.5 μM.	23711832
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM.	22339433
K562	Antiproliferative assay		4 days	Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 μM.	21174434
A375	Antiproliferative assay		4 days	Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50 = 3.9 μM.	21174434
H1299	Antiproliferative assay		4 days	Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50 = 2.4 μM.	21174434
PC3	Antiproliferative assay		4 days	Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50 = 2.1 μM.	21174434
HDMEC	Kinase Assay	0.25/0.5/1 μM	24 h	reduces CK2 kinase activity, vWF expression and secretion	26381437
platelets	Kinase Assay	1/5/10 μM	0.5 h	reduces CK2 kinase activity and platelet aggregation	26381437
UM-SCC1	Growth Inhibition Assay	0.1-30 μM	1-5 d	IC50=4.1 μM	25798061
H1299	Apoptosis Assay	10 μM	72 h	induces apoptosis	25750308
H358	Growth Inhibition Assay	1/5/10 μM	72 h	inhibits cell growth concentration dependently	25750308
Calu-1	Growth Inhibition Assay	1/5/10 μM	72 h	inhibits cell growth concentration dependently	25750308
H1299	Growth Inhibition Assay	1/5/10 μM	72 h	inhibits cell growth concentration dependently	25750308
H28	Growth Inhibition Assay	0.01-30 μM	72 h	IC50=7.2 μM	25422081
A431	Function Assay	10 μM	30 min	attenuates PI3K-Akt-mTOR signaling	22387988
R-LAMA84	Function Assay	3 μM	24 h	reduces CK2 activity	24012109
S-LAMA84	Growth Inhibition Assay	2.5-10 μM	48 h	inhibits cell growth concentration dependently	24012109
R-LAMA84	Growth Inhibition Assay	2.5-10 μM	48 h	inhibits cell growth concentration dependently	24012109
Nalm6	Apoptosis Assay	6/10 μM	48 h	induces apoptosis	24561792
HCT116	Apoptosis Assay	10 μM	24/48 h	induces apoptosis	24686080
MDA-MB-231	Function Assay	2/5/10 μM	4 h	decreases the constitutive phosphorylation of both p-S529-p65 and p-S129-Akt	25153725
MDA-MB-231	Function Assay	2/5/10 μM	4 h	inhibits serine 529 phosphorylation and the expression of IL-6, IL-8	25153725
U87-MG	Growth Inhibition Assay	1/5/10 μM	24/48/72 h	inhibits cell growth both concentration and time dependently	25241897
UM-SCC-1	Clonogenic Assay	0.5-5 μM	14 d	inhibits clonogenic survival and sphere formation	25379016
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
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生物活性

製品説明

特性

First clinical inhibitor of CK2.

Targets

CK2 ^[1]
(Cell-free assay)

1 nM

In Vitro
In vitro	CX-4945 is selective for CK2, as it only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold greater than the IC50 of CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, CX-4945 treatment at 10 μM is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays. CX-4945 exhibits a broad spectrum of antiproliferative activity, and the breast cancer cell lines displays the widest range of sensitivity to CX-4945 with EC50 of 1.71-20.01 μM. The antiproliferative activity of CX-4945 correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. CX-4945 inhibits PI3K/Akt signaling by directly blocking the phosphorylation of Akt at Serine 129 by CK2 rather than through activation of PTEN. CX-4945 treatment causes reduced phosphorylation of p21 (T145), increased levels of total p21 and p27, and induction of caspase 3/7 activity. CX-4945 treatment induces a G2/M cell-cycle arrest in BT-474 cells and a G1 arrest in BxPC-3 cells. CX-4945 inhibits HUVEC proliferation, migration, and tube formation with IC50 of 5.5 μM, 2 μM, and 4 μM, respectively. Under hypoxic conditions in BT-474 and BxPC-3 cells, CX-4945 treatment prevents downregulation of p53 and pVHL and reduces activation of HIF-1α transcription. ^[1] CX-4945 potently inhibits endogenous intracellular CK2 activity with IC50 of 0.1 μM in Jurkat cells. ^[2]
Kinase Assay	CK2 Kinase Assay
Kinase Assay	CX-4945 is added at a volume of 10 μL to a reaction mixture comprising 10 μL of assay dilution buffer (ADB; 20 mM MOPS, pH 7.2, 25 mM β-glycerolphosphate, 5 mM EGTA, 1 mM sodium orthovanadate, and 1 mM dithiothreitol), 10 μL of substrate peptide (RRRDDDSDDD, dissolved in ADB at a concentration of 1 mM), 10 μL of recombinant human CK2 (ααββ-holoenzyme, 25 ng dissolved in ADB). Reactions are initiated by the addition of 10 μL of ATP solution (90% 75 mM MgCl₂, 75 μM ATP (final ATP concentration=15 μM) dissolved in ADB; 10% [γ-³³P]ATP (stock 1 mCi/100 μL; 3000 Ci/mM and maintained for 10 minutes at 30 °C. The reactions are quenched with 100 μL of 0.75% phosphoric acid and then transferred to and filtered through a phosphocellulose filter plate. After washing each well five times with 0.75% phosphoric acid, the plate is dried under vacuum for 5 minutes and, following the addition of 15 μL of scintillation fluid to each well, the residual radioactivity is measured using a Wallac luminescence counter. The IC50 values are derived from eight concentrations of CX-4945 over a range of 0.0001 μM to 1 μM.
細胞実験	細胞株	SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, et al.
	濃度	Dissolved in DMSO, final concentrations ~100 μM
	反応時間	4 days
	実験の流れ	Cells are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with various concentrations of CX-4945. Suspensions cells are seeded and treated on the same day. Following 4 days of incubation, Alamar Blue (20 μL, 10% of volume per well) is added and the cells are further incubated at 37 °C for 4-5 hours. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm is measured.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6 p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail		30683840
	Immunofluorescence	β-catenin E-cadherin / Vimentin		24023938
	Growth inhibition assay	Cell viability		30316146

In Vivo
In Vivo	Oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice daily displays potent antitumor activity in the BT-474 model, with TGI of 88% and 97%, respectively, and 2 of 9 animals in each group showing more than 50% reduction in tumor size compared with the initial tumor volume. In the BxPC-3 model, CX-4945 treatment at 75 mg/kg twice daily shows 93% TGI with 3 animals having no evidence of tumor remaining at the end of the treatment period. ^[1] In PC3 xenograft model, administration of CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg causes tumor growth inhibition with TGI of 19%, 40%, and 86%, respectively. ^[2]
動物実験	動物モデル	Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
	投与量	25 or 75 mg/kg
	投与経路	Oral gavage twice daily

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05817708	Completed	COVID-19	Senhwa Biosciences Inc.	November 7 2022	Phase 1
NCT04668209	Terminated	Coronavirus	University of Arizona\|Senhwa Biosciences Inc.	January 21 2021	Phase 2
NCT04663737	Completed	Covid19	Chris Recknor MD\|Senhwa Biosciences Inc.	December 3 2020	Phase 2
NCT03904862	Suspended	Medulloblastoma Childhood	Pediatric Brain Tumor Consortium\|National Cancer Institute (NCI)\|American Lebanese Syrian Associated Charities (ALSAC)	July 25 2019	Phase 1\|Phase 2
NCT02128282	Completed	Cholangiocarcinoma	Senhwa Biosciences Inc.	June 2014	Phase 1\|Phase 2

参考
[1] Siddiqui-Jain A, et al. Cancer Res, 2010, 70(24), 10288-10298. [2] Pierre F, et al. J Med Chem, 2011, 54(2), 635-654. [3] Siddiqui-Jain A, et al. Mol Cancer Ther, 2012, 11(4), 994-1005. [4] Bliesath J, et al. Cancer Lett, 2012, 322(1), 113-118. + 展開

参考

[4] Bliesath J, et al. Cancer Lett, 2012, 322(1), 113-118.

+ 展開

化学情報

分子量	349.77	化学式	C₁₉H₁₂ClN₃O₂
CAS No.	1009820-21-6	SDF	Download Silmitasertib (CX-4945) SDFをダウンロードする
Smiles	C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4
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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 70 mg/mL ( (200.13 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

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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:
How to reconstitute the compound (S2248) for in vivo uses?

回答
For injection, CX-4945 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, CX-4945 can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.

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):