BO-264 是一种高效，口服活性的转化酸性卷曲螺旋 3 (TACC3) 抑制剂，IC50 为 188 nM，Kd 为 1.5 nM。BO-264 特异性阻断 FGFR3-TACC3 融合蛋白的功能。BO-264 诱导纺锤体检查点依赖的有丝分裂阻滞，DNA 损伤和细胞凋亡 (apoptosis)。BO-264 具有广谱抗肿瘤活性。
货号:ajcx16710
CAS:2408648-20-2
分子式:C18H19N5O3
分子量：353.38
溶解度:DMSO: 50 mg/mL (141.49 mM)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity[1].

[1]. Akbulut O, et al. A Highly Potent TACC3 Inhibitor as a Novel Anti-cancer Drug Candidate. Mol Cancer Ther. 2020 Mar 26. pii: molcanther.0957.2019.