
Chemical Structure
SAR-020106 [1184843-57-9]

SYN-1189
CAS Number1184843-57-9
Product group Chemicals
Estimated Purity>95%
Molecular Weight382.9
Overview
- SupplierSYNkinase
- Product NameSAR-020106 [1184843-57-9]
- Delivery Days Customer10
- CAS Number1184843-57-9
- CertificationResearch Use Only
- Estimated Purity>95%
- Molecular FormulaC19H19ClN6O
- Molecular Weight382.9
- Scientific DescriptionChemical. CAS: 1184843-57-9. Formula: C19H19ClN6O. MW: 382.9. SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3nM on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55nM in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. - SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3nM on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55nM in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo.
- Storage Instruction2°C to 8°C
- UNSPSC51202000