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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-MSC2530818
MSC2530818

Chemical Structure : MSC2530818

CAS No.: 1883423-59-3

MSC2530818 (MSC 2530818;MSC-2530818)

货号: PC-60298Not For Human Use, Lab Use Only.

MSC-2530818 (MSC 2530818, MSC2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM.

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

生物&药学活性

MSC2530818 (MSC 2530818, MSC-2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM.
MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM), and displays good selectivity profile in a 264 kinase panel with exception of GSK3α (IC50=691 nM).
MSC2530818 potently inhibits of phospho-STAT1 S727 in SW620 cells (IC50=8 nM), shows potent inhibition of WNT-dependent transcription in human cancer cell lines.
MSC2530818 demonstrates tumor growth inhibition in an APC mutant SW620 human colorectal carcinoma xenograft model.

物理化学性质&存储条件

分子量 340.811
分子式 C18H17ClN4O
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

[(2S)-2-(4-Chlorophenyl)pyrrolidin-1-yl]-(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone

参考文献

1. Czodrowski P, et al. J Med Chem. 2016 Oct 27;59(20):9337-9349.

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