化合物BO-264 T8492

Product Introduction
Bioactivity


英文名: BO-264

描述: BO-264 是一种有口服活性的转化酸性卷曲螺旋 3 抑制剂，可特异性阻断 FGFR3-TACC3融合蛋白的功能。它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，具有广谱抗肿瘤活性。

体外活性: BO-264 demonstrated superior antiproliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint-dependent mitotic arrest, DNA damage, and apoptosis, while the cytotoxicity against normal breast cells was negligible.?Furthermore, BO-264 significantly decreased centrosomal TACC3 during both mitosis and interphase.?BO-264 displayed potent antiproliferative activity ( 90% have less than 1 μmol/L GI50 value) in the NCI-60 cell line panel compromising of nine different cancer types.?Noteworthy, BO-264 significantly inhibited the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.?Importantly, its oral administration significantly impaired tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increased survival without any major toxicity.?Finally, TACC3 expression has been identified as strong independent prognostic factor in breast cancer and strongly prognostic in several different cancers.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (141.49 mM)


关键字: inhibit | cytotoxicity | antitumor | Fibroblast growth factor receptor | Apoptosis | Inhibitor | TACC3 | spindle | abnormalities | FGFR | ERK1/2 | DNA | phosphorylation | BO-264 | BO 264 | FGFR3-TACC3 | mitotic | damage | anti-proliferative | BO264

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相关库: Anti-Liver Cancer Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途