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

Boiling point:

576.5±50.0 °C(Predicted)

Density 

1.373±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.50 mg/ml; DMSO: 15 mg/ml; Ethanol: 10 mg/ml

form 

A crystalline solid

pka

9.65±0.40(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

(S)-(2-(4-chlorophenyl)pyrrolidin-1-yl)(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone Chemical Properties,Usage,Production

Description

MSC2530818 is an orally bioavailable cyclin-dependent kinase 8 (Cdk8) inhibitor (IC₅₀ = 2.6 nM). It is selective for Cdk8 over a panel of 264 kinases at 1 μM but does inhibit glycogen synthase kinase 3α (GSK3α; IC₅₀ = 691 nM). MSC2530818 inhibits STAT1 phosphorylation in SW620 colorectal cancer cells with an IC₅₀ value of 8 nM. It also inhibits Wnt-dependent transcription in LS 174T, COLO 205, and PA-1 cancer cells (IC₅₀s = 32, 9, and 52 nM, respectively, in luciferase reporter assays). MSC2530818 (50 and 100 mg/kg) reduces tumor growth in a SW620 mouse xenograft model.