Antitumor agent-83 

Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro^[1].

Antitumor agent-83 (Compound 6d) (5-40 µM；24 h) 对 BAX 有激活作用并介导细胞凋亡，以剂量依赖的方式促进细胞色素 C 的释放^[1]。
Antitumor agent-83 对 A549、HCT-116、PC-3、H1581、MDA-MB-231、K562、MV4-11 和 THP-1 肿瘤细胞有显著的抗增殖作用，GI₅₀ 值分别为 2.15 µM、3.31 µM、2.50 µM、2.15 µM、3.98 µM、1.41 µM、2.84 µM、2.18 µM^[1]。
Antitumor agent-83 (1-5 µM；24、48 和 72 h) 以剂量和时间依赖的方式显著降低 A549 细胞的生存能力^[1]。
Antitumor agent-83 (5 µM 和 10 µM；48 h) 以剂量依赖性的方式促进 A549 细胞凋亡^[1]。
Antitumor agent-83 (2.5 µM 和 5 µM；48 h) 以剂量依赖性方式导致 G0/G1 期细胞周期阻滞^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

494.59

C₂₉H₃₀N₆O₂

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• [1]. Zhang Z, et al. Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties. Eur J Med Chem. 2023 Feb 15;248:115076.  [Content Brief]