| Identification | Back Directory | [Name]
(S)-(2-(4-chlorophenyl)pyrrolidin-1-yl)(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone | [CAS]
1883423-59-3 | [Synonyms]
CPD1540
MSC2530818
(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-2H-pyrazolo[3,4-b]pyridin-5-yl)methanone
Methanone, [(2S)-2-(4-chlorophenyl)-1-pyrrolidinyl](3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)- | [Molecular Formula]
C18H17ClN4O | [MDL Number]
MFCD31382190 | [MOL File]
1883423-59-3.mol | [Molecular Weight]
340.81 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [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. |
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