Silmitasertib (CX-4945) sodium salt

目录号：S0707 Purity: 99.95%

Silmitasertib (CX-4945) sodium salt是一种有效的、口服可生物利用的、选择性的 casein kinase 2 (CK2) 的抑制剂，对CK2α和CK2α'的IC50值为1 nM。

Silmitasertib (CX-4945) sodium salt Chemical Structure

CAS: 1309357-15-0

规格	价格	库存
10mM (1mL in DMSO)	RMB 1570	现货
5mg	RMB 970.55	现货
25mg	RMB 2970.89	现货
100mg	RMB 4832.1	现货
1g	RMB 12039.3	现货
更大包装有超大折扣
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客户使用Selleck的Silmitasertib (CX-4945) sodium salt发表文献61篇

产品质控

批次：纯度： 99.95%

99.95

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Casein Kinase抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

Silmitasertib (CX-4945) sodium salt是一种有效的、口服可生物利用的、选择性的 casein kinase 2 (CK2) 的抑制剂，对CK2α和CK2α'的IC50值为1 nM。

靶点

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (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

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

参考文献

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

化学信息&溶解度

分子量	371.75	分子式	C₁₉H₁₁ClN₃NaO₂
CAS号	1309357-15-0	SDF	--
Smiles	C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)[O-])C4=C2C=CN=C4.[Na+]
储存条件(自收到货起)	3年 -20°C 粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年 -20°C 粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 37 mg/mL ( (99.52 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 5 mg/mL

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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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):