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Product Details
Synonyms SAR020106
Product Type Chemical
Formula C19H19ClN6O
MW 382.9
CAS 1184843-57-9
Purity Chemicals ≥95%
Appearance Solid.
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
Shipping AMBIENT
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.
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF

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.

Product References
  1. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106: M.I. Walton, et al.; Mol. Cancer Ther. 9, 89 (2010)
  2. 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)
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