SR-1277

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SR-1277 

SR-1277 是一种有效、选择性和 ATP 竞争性的 CK1δ/ε 抑制剂,IC50 值分别为 49 nM 和 260 nM。SR-1277 还抑制 FLT3CDK4/cyclin D1CDK6/cyclin D3CDK9/cyclin KIC50 值分别为 305 nM,1340 nM,311 nM 和 109 nM。SR-1277 可用于癌症研究。

SR-1277

SR-1277 Chemical Structure

CAS No. : 1446715-47-4

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生物活性

SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer[1].

IC50 & Target[1]

CKIδ

49 nM (IC50)

CKIϵ

260 nM (IC50)

体外研究
(In Vitro)

SR-1277 exhibits antiproliferative effects in A375 cells, with an EC50 of 22 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SR-1277 (1 mg/kg; i.v.) exhibits Cmax (1.2 μM), Cl (2.8 ml/min/kg), AUC(1.26 μM•h), T1/2 (1.42 h) and brain penetration (24%) in mice[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

477.50

Formula

C21H19N9O3S

CAS 号

1446715-47-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Bibian M, et, al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80.

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