MSC2530818 , 10mMinDMSO , 1883423-59-3

CAS NO.：1883423-59-3

Empirical Formula: C18H17ClN4O

Molecular Weight: 340.81

MDL number:

PRODUCT Properties

• 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

Description and Uses

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.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning