MSC2530818

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 3alpha (GSK3alpha, 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.Formal Name: [(2S)-2-(4-chlorophenyl)-1-pyrrolidinyl](3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-methanone. CAS Number: 1883423-59-3. Molecular Formula: C18H17ClN4O. Formula Weight: 340.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.50 mg/ml, DMSO: 15 mg/ml, Ethanol: 10 mg/ml. lambdamax: 223 nm. SMILES: CC1=NNC2=NC=C(C(N3CCC[C@@]3([H])C4=CC=C(Cl)C=C4)=O)C=C21. InChi Code: InChI=1S/C18H17ClN4O/c1-11-15-9-13(10-20-17(15)22-21-11)18(24)23-8-2-3-16(23)12-4-6-14(19)7-5-12/h4-7,9-10,16H,2-3,8H2,1H3,(H,20,21,22)/t16-/m0/s1. InChi Key: ODRITQGYYWHQGM-INIZCTEOSA-N.