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MSC2530818

Chemical Structure : MSC2530818

CAS No.: 1883423-59-3

MSC2530818 (MSC 2530818;MSC-2530818)

Catalog No.: PC-60298Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MSC2530818 (MSC 2530818, MSC-2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM.
MSC2530818 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).
MSC2530818 potently inhibits of phospho-STAT1 S727 in SW620 cells (IC50=8 nM), shows potent inhibition of WNT-dependent transcription in human cancer cell lines.
MSC2530818 demonstrates tumor growth inhibition in an APC mutant SW620 human colorectal carcinoma xenograft model.

Physicochemical Properties

M.Wt 340.811
Formula C18H17ClN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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