BO-264,2408648-20-2

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BO-264

CAS No. : 2408648-20-2

MCE 国际站：BO-264

产品活性：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，K_d 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。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：FGFR  |  Apoptosis

In Vitro: BO-264 (500 nM; 48 hours; JIMT-1 cells) treatment induces a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells as assessed by Annexin V/PI staining.
BO-264 (500 nM; 24 hours; RT112 cells) treatment decreases ERK1/2 phosphorylation, which is a marker for activated FGFR signaling along with a strong mitotic arrest.
BO-264 inhibits cell viability with IC₅₀ values of 190 nM, 160 nM, 120 nM, 130 nM and 360 nM for JIMT-1, HCC1954, MDA-MB-231, MDA-MB-436 and CAL51, respectively. BO-264 specifically targets breast cancer cells while sparing normal cells. BO-264 treatment significantly reduces the average colony number of JIMT-1 cells.
BO-264 inhibits the viability of cancer cells with FGFR3-TACC3 fusion with IC₅₀ values of 0.3 μM and 3.66 μM for RT112 and RT4, respectively.
BO-264 exhibits a remarkable anti-cancer activity against more than 90% of the NCI267 60 human cancer cell lines representing nine different subpanels with GI₅₀ values less than 1 μM.
BO-264 induces mitotic arrest (prominent induces p-Histone H3 (Ser10)), apoptosis (cleaved PARP) and DNA damage, causes aberrant spindle formation and reduces centrosomal localization of TACC3 in JIMT-1 cells.

In Vivo: BO-264 (25 mg/kg; oral administration; daily; for 3-4 weeks; female nude mice) treatment shows a significant suppression of tumor growth. BO-264 is well tolerated since treatment does not causes a significant body weight loss and organ toxicity.

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