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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-SEL120-34A
SEL120-34A

Chemical Structure : SEL120-34A

CAS No.: 1609522-33-9

SEL120-34A (Romaciclib, SEL 120-34A, SEL120)

货号: PC-61658Not For Human Use, Lab Use Only.

Romaciclib (SEL120-34A) is an ATP-competitive, selective, orally active CDK8/19 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Romaciclib (SEL120-34A) is an ATP-competitive, selective, orally active CDK8/19 inhibitor that inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50 of 4.4 nM and 10.4 nM, respectively.
SEL120-34A shows no significant inhibition on other members of the CDK family (200-fold over CDK9).
SEL120-34A inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits IFN- responsive genes expression in vitro.
SEL120-34A exhibits complete inhibitions of STAT1 S727 and STAT5 S726 in Colo-205 CRC xenograft tissues in mice (60mg/kg).

物理化学性质&存储条件

分子量 414.145
分子式 C15H18Br2N4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7,8-Dibromo-9-methyl-2-piperazin-1-yl-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline

参考文献

1. Rzymski T, et al. Oncotarget. 2017 May 16;8(20):33779-33795.

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