Ceralasertib (AZD6738) (C09-0822-602)

InformationCeralasertib (AZD6738) is an orally active, and selectiveATRkinase inhibitor withIC50of 1 nM. Phase 1/2.In vitroIn 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. 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.In vivoIn 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. In nude mice bearing LoVo xenografts, a combination of AZD6738 (50/u2009mg/kg)/u2009+/u2009IR (2/u2009Gy) avoids toxicity while still maintaining efficacy.Cell Datacell lines：MDA-MB-231 cell lineConcentrations：~30 μMIncubation Time：48 hPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C20H24N6O2S Molecular Weight: 412.51