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Silmitasertib (CX-4945)?sodium salt

Silmitasertib (CX-4945)?sodium salt是一種有效的、口服可生物利用的、選擇性的 casein kinase 2 (CK2) 的抑制劑，對CK2α和CK2α'的IC50值為1 nM。

Silmitasertib (CX-4945)?sodium salt Chemical Structure

Silmitasertib (CX-4945)?sodium salt Chemical Structure

CAS: 1309357-15-0

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1570 現(xiàn)貨
5mg 970.55 現(xiàn)貨
25mg 2970.89 現(xiàn)貨
100mg 4832.1 現(xiàn)貨
1g 12039.3 現(xiàn)貨
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Silmitasertib (CX-4945)?sodium salt相關產(chǎn)品

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Silmitasertib (CX-4945)?sodium salt是一種有效的、口服可生物利用的、選擇性的 casein kinase 2 (CK2) 的抑制劑，對CK2α和CK2α'的IC50值為1 nM。
靶點
CK2α [1]
(Cell-free assay)		 CK2α' [1]
(Cell-free assay)
1 nM 1 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

化學信息&溶解度

分子量 371.75 分子式

C19H11ClN3NaO2
CAS號 1309357-15-0 SDF --
Smiles C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)[O-])C4=C2C=CN=C4.[Na+]
儲存條件(自收到貨起) 3年 -20°C 粉狀

體外溶解度
批次：

DMSO : 37 mg/mL ( (99.52 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 5 mg/mL (13.44 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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