计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。An ATP-competitive CK2 protein kinase inhibitor.
Information
Silmitasertib (CX-4945) 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 p
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. CX-4945 potently inhibits endogenous intracellular CK2 activity with IC50 of 0.1 μM in Jurkat cells.
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. 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.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~100 μM
Incubation Time：4 days
Powder Purity:≥99%
规格
别名
西米他赛特 (CX-4945)
英文别名
5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Silmitasertib (CX-4945)
生化机理
Silmitasertib（CX-4945）是一种强效的酪蛋白激酶 2（CK2）选择性抑制剂，在无细胞试验中的 IC50 为 1 nM，对 Flt3、Pim1 和 CDK1 的抑制作用较弱（在细胞试验中无活性）。Silmitasertib 能诱导自噬并促进细胞凋亡。1/2阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
酪蛋白激酶 IIα 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4
分子量
349.77
Reaxy-Rn
13112605
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13112605&ln=
技术文档
高级数据
产品属性
| ALogP | 4.4 |
|---|
关联靶点（人）
DYRK1B
Tchem
双特异性酪氨酸磷酸化调节激酶 1B(Dual specificity tyrosine-phosphorylation-regulated kinase 1B)
(3 活性数据)
DYRK1A
Tchem
双特异性酪氨酸磷酸化调节激酶 1A(Dual specificity tyrosine-phosphorylation-regulated kinase 1A)
(3 活性数据)
CSNK2A2
Tchem
酪蛋白激酶 II 亚基 α'(Casein kinase II subunit alpha')
(4 活性数据)
DAPK3
Tchem
死亡相关蛋白激酶 3(Death-associated protein kinase 3)
(3 活性数据)
CSNK2A1
Tchem
酪蛋白激酶 II 亚基 α(Casein kinase II subunit alpha)
(16 活性数据)
HIPK3
Tchem
同源域相互作用蛋白激酶 3(Homeodomain-interacting protein kinase 3)
(1 活性数据)
PIM1
Tchem
丝氨酸/苏氨酸蛋白激酶 pim-1(Serine/threonine-protein kinase pim-1)
(1 活性数据)
MAPKAPK3
Tchem
MAP激酶活化蛋白激酶3(MAP kinase-activated protein kinase 3)
(1 活性数据)
PRKAG2
Tchem
5'-AMP活化蛋白激酶亚基γ-2(5'-AMP-activated protein kinase subunit gamma-2)
(1 活性数据)
CLK3
Tchem
双特异性蛋白激酶 CLK3(Dual specificity protein kinase CLK3)
(1 活性数据)
CLK1
Tchem
双特异性蛋白激酶 CLK1(Dual specificity protein kinase CLK1)
(1 活性数据)
CLK2
Tchem
双特异性蛋白激酶 CLK2(Dual specificity protein kinase CLK2)
(4 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
此产品的引用文献
溶液计算器
常见问题
「Moligand?」是什么？
「Moligand?」是阿拉丁科学的高端产品线之一，专为多个工作流程中的高纯度应用而设计。与同类工作流程中的标准级别相比，「Moligand?」产品通常具有更严格的规格、更严谨的 QC 以及更强的批间一致性。
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1009820-21-6，分子式为 C19H12ClN3O2，分子量为 349.77 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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