AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR. In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296 levels in a concentration-dependent manner. Prolonged exposure with AZ20 increases H2AX pan-nuclear staining, indicative of replication stress. AZ20 induces growth inhibition and cell death and its profile of activity is distinctly when compares with other cytotoxic agents. in vivo,AZ20 induces significant tumour growth inhibition at well tolerated doses.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
Abstract 1823: AZ20, a novel potent and selective inhibitor of ATR kinase with in vivo antitumour activity.
Foote KM, et al. J Med Chem. 2013 Mar 14;56(5):2125-38. PMID: 23394205.
|Related ATM/ATR Products|
Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models
Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity.
Candesartan Cilexetil is a specific nonpeptide Ang II receptor (ATR) antagonist and the procompound of candesartan which is an ATR antagonist with an IC50 of 15 μg/kg.
VE-822 is an ATR inhibitor with IC50 of 19 nM.
CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.