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.
|Source||Sci Rep (2017). Figure 1. AZ20|
|Method||flow cytometry analyses|
|Cell Lines||AML cell lines|
|Incubation Time||24 h|
|Results||Based on the samples tested, AZ20 sensitivity appeared to be similar between these two groups (p = 0.8, calculated using the Mann-Whitney U-test).|
|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.
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