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.
Nat Commun. 2019 Dec 20;10(1):5799.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 70 mg/mL|
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AZ32 is an orally bioavailable and blood-brain barrier-(BBB)penetrating inhibitor of ATM with IC50 of <6.2 nM and 0.31 μM for ATM enzyme in cell.
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