MSC2504877
Modify Date: 2024-04-09 22:10:50
MSC2504877 structure
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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 MSC2504877MSC2504877 (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 |
| InChIKey | MPXAEYSGFKRDQM-UHFFFAOYSA-N |
| SMILES | Cc1ccc2c(=O)[nH]c(-c3ccc(C(C)(C)O)cc3)cn12 |