SAR-020106

SAR-020106 - Names and Identifiers

Name	(R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile
Synonyms	SAR20106 SAR20106 SAR020106 SAR 20106 SAR020106 SAR-020106 SAR 20106 SAR 020106 (R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile 5-[(8-Chloro-3-isoquinolinyl)amino]-3-[(1R)-2-(dimethylamino)-1-methylethoxy]-2-pyrazinecarbonitrile 2-Pyrazinecarbonitrile, 5-[(8-chloro-3-isoquinolinyl)amino]-3-[(1R)-2-(dimethylamino)-1-methylethoxy]-
CAS	1184843-57-9

SAR-020106 - Physico-chemical Properties

Molecular Formula	C19H19ClN6O
Molar Mass	382.85
Solubility	DMSO
Storage Condition	-20℃
Use	SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.
In vitro study	SAR-020106 abolishing the etoposide-induced G2 phase cell arrest, the IC50 was 55 n in HT29 cells. In several colon cancer cell lines in vitro, the cell killing ability of gemcitabine and SNS38 was significantly enhanced, and this effect was dependent on p53. SAR-020106 inhibits the autophosphorylation of CHK1 at the S296 site induced by cytotoxic drugs and blocks the phosphorylation of CDK1 at The Y5 position.
In vivo study	SAR-020106 potentiates the antitumor activity of irinotecan and gemcitabine in vivo with little toxic effect. Although its oral bioavailability in mice is small (F = 5%), when 40 mg/kg is injected by intraperitoneal injection, SAR-020106 was sufficient to inhibit CHK1 in tumor tissue, inhibiting irinotecan-induced CHK1 autophosphorylation at the S296 site. In the SW620 xenograft tumor mouse model, administration of SAR-020106 alone has no activity, and when SAR-020106 and irinotecan are used in combination, SAR-020106 can enhance the antitumor activity of this genotoxic drug.

SAR-020106 - Reference

Reference

1. Walton MI, et al. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010;9(1):89-100.2. Reader JC, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011;54(24):8328-8342.

SAR-020106 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.612 ml	13.06 ml	26.12 ml
5 mM	0.522 ml	2.612 ml	5.224 ml
10 mM	0.261 ml	1.306 ml	2.612 ml
5 mM	0.052 ml	0.261 ml	0.522 ml

Last Update：2024-01-02 23:10:35

SAR-020106 - Reference Information

biological activity	SAR-020106 is an ATP-competitive, potent and selective CHK1 inhibitor with an IC50 of 13.3 nM.
Target	Value
Chk1 (Cell-free assay)	13.3 nM

Last Update：2024-04-09 21:32:10