1184843-57-9
Chemical Structure
SAR-020106
- CAS No.: 1184843-57-9
- Formula:C19H19ClN6O
- Molecular Weight:382.85
IUPAC Name: (R)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile
InChIKey: SRBJWIBAMIKCMV-GFCCVEGCSA-N
SMILES: N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C
Biological Activity: SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents[1][2].
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SAR-020106 | 98.04% | SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
