MSC2504877|MSC-2504877;MSC 2504877

Cas No.:	1460286-21-8
Chemical Name:	MSC2504877
Synonyms:	MSC2504877;3-(4-(2-Hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one;3-[4-(2-hydroxypropan-2-yl)phenyl]-6-methyl-2H-pyrrolo[1,2-a]pyrazin-1-one
SMILES:	OC(C)(C)C1C=CC(=CC=1)C1=CN2C(C)=CC=C2C(N1)=O
Formula:	C₁₇H₁₈N₂O₂
M.Wt:	282.337024211884
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

MSC2504877 (MSC-2504877) a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM); increased AXIN2 protein levels and decreased β-catenin levels in APC mutant COLO320DM colorectal tumour cells, suppressed canonical Wnt signalling in SW480 cell line, inhibits the growth of APC mutant colorectal tumour cells; enhances G1 cell cycle arrest and cellular senescence in tumour cells when combined with CDK4/6 inhibitor Palbociclib, suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of pRb; Palbociclib plus MSC2504877 combination suppresses hyperproliferation in Apc defective cells in vivo.

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