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SynKinase
SAR-020106
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | SAR020106 |
| Product Type | Chemical |
| Properties | |
| 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. |
| InChi Key | SRBJWIBAMIKCMV-GFCCVEGCSA-N |
| 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. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
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
- 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)
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