 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 1352226-88-0 |
| Molecular formula(MF) | C20H24N6O2S |
| Molecular Weight(MW): | 412.51 |
| Alias |
| In vitro | DMSO | 82 mg/mL (198.78 mM) |
|---|---|---|
| Ethanol | 41 mg/mL warmed (99.39 mM) | |
| Water | <1 mg/mL | |
| In vivo | 10% DMSO+40% propylene glycol+ddH2O | 10mg/mL |
| Description | AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. | ||
|---|---|---|---|
| Targets |
|
||
| In vitro |
In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with cisplatin to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. [2] |
||
| In vivo | In nude mice bearing H460 and H23 tumors, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with cisplatin causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. [3] |