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product name SAR-020106


Description: SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM on isolated human enzyme. This compound abrogates an etoposide-induced G2 arrest with an IC50 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.  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. 

References: Radiother Oncol. 2013 Jul;108(1):24-31; Int J Radiat Oncol Biol Phys. 2013 Mar 15;85(4):1110-8.



Molecular Weight (MW)

382.85 
Formula

C19H19ClN6
CAS No.

1184843-57-9 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 20 mg/mL (52.2 mM) 
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)

 
Synonyms

 

other peoduct :

In Vitro

In vitro activity


Kinase Assay:


Cell Assay

In Vivo  
Animal model  
Formulation & Dosage  
References  

EW-7200

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Author: Sodium channel