MSC-2530818( MSC 2530818 | MSC2530818 )

Catalog No. M12925 CAS No. 1883423-59-3

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Product Name

MSC-2530818
Note

Research use only, not for human use.
Brief Description

MSC-2530818 (MSC 2530818, MSC2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM.
Description

MSC-2530818 (MSC 2530818, MSC2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM; binds to CDK8 and CDK19 with similar affinity (4 nM), and displays good selectivity profile in a 264 kinase panel with exception of GSK3α (IC50=691 nM); potently inhibits of phospho-STAT1 S727 in SW620 cells (IC50=8 nM), shows potent inhibition of WNT-dependent transcription in human cancer cell lines; demonstrates tumor growth inhibition in an APC mutant SW620 human colorectal carcinoma xenograft model.
In Vitro

——
In Vivo

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Synonyms

MSC 2530818 | MSC2530818
Pathway

Angiogenesis
Target

CDK
Recptor

CDK
Research Area

Cancer
Indication

——

CAS Number

1883423-59-3
Formula Weight

340.811
Molecular Formula

C18H17ClN4O
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 125 mg/mL 366.77 mM
SMILES

O=C(N1[C@H](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3
Chemical Name

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

1. Czodrowski P, et al. J Med Chem. 2016 Oct 27;59(20):9337-9349.

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