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Product Description:
Product Name: MSC2530818 CAS NO: 1883423-59-3
Synonyms:
(S)-(2-(4-chlorophenyl)pyrrolidin-1-yl)(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone;
[(2S)-2-(4-Chlorophenyl)pyrrolidin-1-yl]-(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone;
CPD1540;
Chemical & Physical Properties:
Appearance: Crystalline solid
Assay :≥98.0%
Boiling Point: 576.5±50.0℃ (Predicted)
Density: 1.373±0.06 g/cm3 (Predicted)
PKa: 9.65±0.40 (Predicted)
MSC2530818 is a CDK8 inhibitor with an IC50 of 2.6 nM. It has good kinase selectivity, biochemical and cellular potency, microsomal stability, and biooral activity. MSC2530818 binds CDK8 and CDK19 with a similar affinity and effectively inhibits phospho-STAT1 in SW620 colorectal cancer cells. MSC2530818 showed acceptable and good pharmacokinetic properties in all animal species tested (mouse, rat, dog). It can effectively reduce the tumor growth rate in human SW620 colorectal carcinoma transplantation model.
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