1460286-21-8
1460286-21-8 structure
- Name: MSC2504877
- Chemical Name: MSC2504877
- CAS Number: 1460286-21-8
- Molecular Formula: C17H18N2O2
- Molecular Weight: 282.343
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2020-01-20 14:10:56
- Modify Date: 2024-04-09 22:10:50
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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.
| Name | MSC2504877 |
|---|
| 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 |
| Molecular Formula | C17H18N2O2 |
|---|---|
| Molecular Weight | 282.343 |