ST-401 

ST-401, a microtubule-targeting agent (MTA), is a brain-penetrant microtubule (MT) assembly inhibitor. ST-401 disrupts microtubule (MT) function through gentle and reverisible reduction in MT assembly that triggers mitotic delay and cell death in interphase. ST-401 shows a potent antitumor activity^[1].

ST-401 是一种混合分子，将仲醇和喹啉结合在一个结构中。ST-401 竞争 89% 的 [3H]秋水仙碱与微管蛋白的结合。在浊度测定中，ST-401 抑制微管蛋白组装，IC₅₀ 为 1.1 µM。在测量游离微管蛋白释放的沉淀测定中，ST-401 抑制微管蛋白组装，IC₅₀ 值为 3.2 µM^[1]。
ST-401 在大多数人类癌细胞系中表现出类似的低纳摩尔抗肿瘤活性，包括六种神经胶质瘤系（SF-268、SF-295、SF-539、SNB-19、SNB-75 和 U251：IC50 为 23-69 nM）^[1]。
ST-401 在 PD-神经胶质瘤中表现出低纳摩尔抗肿瘤活性（IC50：24-47 nM）^[1]。
ST-401（72 小时）降低了 MGG8 和 T98G 细胞中的整体细胞活力，IC₅₀ 相当（分别为 14 和 36 nM）^[1]。

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

ST-401 (20 mg/kg；腹腔注射；每日两次；每周 5 天，持续 4 周) 在异种移植侧腹肿瘤小鼠模型中表现出显着的抗肿瘤活性且无过度毒性^[1]。

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

352.43

C₂₄H₂₀N₂O

2419942-78-0

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Eric A Horne, et al. A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis. Neurooncol Adv. 2020 Dec 3;3(1):vdaa165.  [Content Brief]