|Solubility||Soluble in DMSO.|
|Declaration||Manufactured by SynKinase.|
|Other Product Data||
Target: EGFR - HER2 | Kinase Group: RTK | Substrate: Tyrosine
Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||+4°C|
|Use/Stability||Stable for at least 1 year after receipt when stored at +4°C.|
|Product Specification Sheet|
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.
- The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106: M.I. Walton, et al.; Mol. Cancer Ther. 9, 89 (2010)
- The Chk1 inhibitor SAR-020106 sensitizes human glioblastoma cells to irradiation, to temozolomide, and to decitabine treatment: I. Patties, et al.; J. Exp. Clin. Cancer Res. 38, 420 (2019)