MSC2504877

Modify Date: 2024-04-09 22:10:50

MSC2504877 Structure
MSC2504877 structure
 Common Name MSC2504877
CAS Number 1460286-21-8 Molecular Weight 282.343
Density N/A Boiling Point N/A
Molecular Formula C17H18N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MSC2504877


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.

 Names

Name MSC2504877

 MSC2504877 Biological Activity

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.
References References 1. Menon M, et al. Sci Rep. 2019 Jan 17;9(1):201. View Related Products by Target PARP

 Chemical & Physical Properties

Molecular Formula C17H18N2O2
Molecular Weight 282.343
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Chemsrc provides MSC2504877(CAS#:1460286-21-8) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of MSC2504877 are included as well.>> amp version: MSC2504877

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