SAR-020106

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP29578CAS No. ：1184843-57-9Purity：98%

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CAS No.	1184843-57-9	Cat. No.	BCP29578
Name	SAR-020106
Synonyms	SAR020106; SAR 020106; SAR20106; SAR20106; SAR 20106;
SMILES	N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C
Chemical Name
Formula	C19H19ClN6O	M. Wt	382.85
Purity	98%	Storage	Store at 4-8°C
Description	SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L 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 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility.