中文名：Ceralasertib (AZD6738)
英文名：Ceralasertib (AZD6738)
纯度：Moligand™，≥99%
货号：C413815
Cas号：1352226-88-0
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
Ceralasertib (AZD6738) is an orally active, and selectiveATRkinase inhibitor withIC50of 1 nM. Phase 1/2.
Targets
ATR (Cell-free assay) 1 nM
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. 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 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. In nude mice bearing LoVo xenografts, a combination of AZD6738 (50\u2009mg/kg)\u2009+\u2009IR (2\u2009Gy) avoids toxicity while still maintaining efficacy.
Cell Research(from reference)
Cell lines：H23, H460, A549, and H358 cells
Concentrations：~30 μM
Incubation Time：48 h
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关键字： NSC780249 ; s7693 ; Z3952965739 ; (R)-3-methyl-4-(6-(1-((R)-S-methylsulfonimidoyl)cyclopropyl)-2-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl)morpholine
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