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。

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC 50 of 188 nM and a K d 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.

Solid

IC50: 188 nM (Transforming acidic coiled-coil 3 (TACC3))
Kd: 1.5 nM (TACC3)

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

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 50 mg/mL (141.49 mM; Need ultrasonic)配制储备液