Silmitasertib (CX-4945) sodium salt

Silmitasertib (CX-4945) sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.

CAS No. 1309357-15-0

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 70500	国内在庫あり
100mg	JPY 145500	国内在庫なし(納期7~10日)
1g	JPY 448500	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（61）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Silmitasertib (CX-4945) sodium salt関連製品

関連ターゲット	CK1 CK2	もっと見る
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
LNCAP	Apoptosis assay	>10 uM	1 to 2 days	Induction of apoptosis in human LNCAP cells assessed as increase in caspase3 activation at >10 uM after 1 to 2 days	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of survivin expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	1 to 10 uM	12 hrs	Inhibition of CK2 in human LNCAP cells assessed as androgen receptor nuclear translocation at 1 to 10 uM after 12 hrs by Alexa Fluor 488 staining based fluorescence assay	22832316
LNCAP	Function assay	1 to 10 uM	1 day	Inhibition of CK2 in human LNCAP cells assessed as DHT-mediated androgen receptor activation at 1 to 10 uM after 1 day by luciferase assay	22832316
LNCAP	Function assay	10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent PSA mRNA level at 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent TMPRSS2 mRNA level at 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	1 to 10 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of DHT-induced androgen receptor dependent TMPRSS2 mRNA expression at 1 to 10 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	3 uM	8 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor dependent DHT-induced PSA mRNA expression at 3 uM after 8 hrs by real time PCR analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Apoptosis assay	30 uM	72 hrs	Induction of apoptosis in human LNCAP cells at 30 uM after 72 hrs by AnnexinV staining based fluorescent microscopy	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of cytosolic protein level at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Downregulation of CK2alpha expression in human LNCAP cells assessed as reduction of nuclear protein level at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of p21 phosphorylation at threonine145 at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of Akt phosphorylation at Ser473 at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as reduction of XIAP expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2alpha in human LNCAP cells assessed as induction of CHOP expression at 10 uM after 12 to 24 hrs by Western blot analysis	22832316
LNCAP	Function assay	10 uM	12 to 24 hrs	Inhibition of CK2 in human LNCAP cells assessed as reduction of androgen receptor nuclear translocation at 10 uM after 12 to 24 hrs by HCS analysis	22832316
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
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	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	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	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
HeLa	Function assay	8 uM	12 hrs	Inhibition EGFP-CK2alpha (unknown origin) expressed in human HeLa cells induction of EGFP-CK2alpha translocation from nucleoli to nuclear matrix and cytoplasm at 8 uM after 12 hrs by Hoechst-33342-staining based microscopy	30689946
A549	Function assay	10 uM		Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method	24012124
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of COL1 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of COL1 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of CCN2 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as down-regulation of CCN2 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of ACTA2 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of ACTA2 protein expression at 10 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	1 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of MYH11 protein expression at 1 nM by Western blot analysis	ChEMBL
pulmonary smooth muscle cells	Function assay	10 nM		Inhibition of casein kinase-2/Nkx2-5 in human pulmonary smooth muscle cells assessed as up-regulation of MYH11 protein expression at 10 nM by Western blot analysis	ChEMBL
MIAPaCa2	Antiproliferative assay		4 days	Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50=1.1μM	21174434
PC3	Antiproliferative assay		4 days	Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50=2.1μM	21174434
HCT116	Antiproliferative assay		4 days	Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50=2.2μM	21174434
H1299	Antiproliferative assay		4 days	Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50=2.4μM	21174434
Jurkat	Antiproliferative assay		4 days	Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50=2.5μM	21174434
A549	Antiproliferative assay		4 days	Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50=3μM	21174434
A375	Antiproliferative assay		4 days	Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50=3.9μM	21174434
BxPC3	Antiproliferative assay		4 days	Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50=4.4μM	21174434
LNCAP	Antiproliferative assay		4 days	Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50=4.7μM	21174434
K562	Antiproliferative assay		4 days	Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50=5.3μM	21174434
MDA-MB-231	Antiproliferative assay		4 days	Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50=6.4μM	21174434
MCF7	Antiproliferative assay		4 days	Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50=8.9μM	21174434
Hs 578T	Antiproliferative assay		4 days	Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50=13.1μM	21174434
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=5.2μM	22339433
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50=6.5μM	22339433
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50=8.2μM	22339433
LNCAP	Cytotoxicity assay		4 days	Cytotoxicity against human LNCAP cells assessed as cell viability after 4 days by CCK8 method, IC50=4.59μM	22832316
MV4-11	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50=3μM	23711832
U937	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50=4.2μM	23711832
Jurkat	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50=4.5μM	23711832
K562	Antiproliferative assay		1 to 3 days	Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50=7μM	23711832
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50=9.9μM	26850376
Sf21 insect	Function assay		20 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<0.003μM	29559278
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis, IC50=1μM	30689946
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as decrease in alpha-catenin phosphorylation at Ser641 after 24 hrs by Western blot analysis, EC50=1μM	30689946
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as reduction in STAT3 phosphorylation at Y705 after 24 hrs by Western blot analysis, EC50=5.3μM	30689946
Vero E6	Function assay		48 hrs	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=3.89045μM	32353859
Jurkat	Function assay			Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50=0.1μM	21174434
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=1.8μM	24681986
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
pulmonary smooth muscle cells	Function assay			Inhibition of de-differentiation of human pulmonary smooth muscle cells assessed as reduction in contractile to synthetic forms change, EC=0.001μM	ChEMBL
Jurkat T	Function assay			Modulation of Endogenous Assay: The human leukemia Jurkat T-cell line was maintained in RPMI 1640 (Cambrex) supplemented with 10% fetal calf serum and 50 ng/ml Geutamycin. Before treatment cells were washed, resuspended at a density of about 106 cells/mil, IC50=0.1μM	ChEMBL
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生物活性

製品説明

Silmitasertib (CX-4945) sodium salt is a potent, orally bioavailable and selective inhibitor of casein kinase 2 (CK2) with IC50 of 1 nM against CK2α and CK2α'.

Targets

CK2α ^[1] (Cell-free assay)	CK2α' ^[1] (Cell-free assay)
1 nM	1 nM

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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	Recruiting	Medulloblastoma Childhood	Pediatric Brain Tumor Consortium\|St. Jude Children''s Research Hospital\|National Cancer Institute (NCI)	July 25 2019	Phase 1\|Phase 2
NCT02128282	Completed	Cholangiocarcinoma	Senhwa Biosciences Inc.	June 2014	Phase 1\|Phase 2

参考
[1] Adam Siddiqui-Jain, et al. Cancer Res. 2010 Dec 15;70(24):10288-98.

参考

[1] Adam Siddiqui-Jain, et al. Cancer Res. 2010 Dec 15;70(24):10288-98.

化学情報

分子量	371.75	化学式	C₁₉H₁₁ClN₃NaO₂
CAS No.	1309357-15-0	SDF	--
Smiles	C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)[O-])C4=C2C=CN=C4.[Na+]
保管	3 years -20°C powder	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 years -20°C powder	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 : 37 mg/mL ( (99.52 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 : 5 mg/mL

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。

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):