英文名称：AZD6738
产品别名：AZD-6738
质量标准：98%
CAS：1352226-88-0
分子式：C20H24N6O2S
分子量：412.51
生物活性：
AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.
IC50 value: 1 nM
Target: ATR kinase
in vitro: AZD6738 is an orally active and bioavailable ATR kinase inhibitor. AZD6738 induces cell death and senescence in non-small cell lung cancer (NSCLC) cell lines. AZD6738 potentiates the cytotoxicity of cisplatin and gemcitabine in NSCLC cell lines with intact ATM kinase signaling, and potently synergizes with cisplatin in ATM-deficient NSCLC cells. AZD6738 inhibits ATR kinase activity and impairs viability of NSCLC. [1]
in vivo: In contrast to expectations, daily administration of AZD6738 and ATR kinase inhibition for 14 consecutive days is tolerated in mice and enhances the therapeutic efficacy of cisplatin in xenograft models. Remarkably, the combination of cisplatin and AZD6738 resolves ATM-deficient lung cancer xenografts. [1]
相关文献：
[1]. Vendetti FP, et al. The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of cisplatin to resolve ATM-deficient non-small cell lung cancer in vivo. Oncotarget. 2015 Oct 27. doi: 10.18632/oncotarget.6247.
