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MSC2504877

Chemical Structure : MSC2504877

CAS No.: 1460286-21-8

MSC2504877 (MSC-2504877;MSC 2504877;M2912)

Catalog No.: PC-36007Not For Human Use, Lab Use Only.

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).

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

Biological Activity

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).
MSC2504877 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.
MSC2504877 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.

Physicochemical Properties

M.Wt 282.343
Formula C17H18N2O2
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

3-(4-(2-hydroxypropan-2-yl)phenyl)-6-methylpyrrolo[1,2-a]pyrazin-1(2H)-one

References

1. Menon M, et al. Sci Rep. 2019 Jan 17;9(1):201.

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