|3-(4-甲氧基苯基)-N-(2-吗啉嘧啶-4-基)异恶唑-5-胺|CsnPharm

CAS No.: 2408648-20-2

BO-264 Catalog No. CSN25666

BO-264 is a highly TACC3 inhibitor with IC50 value of 188nM. It significantly decreased centrosomal TACC3 during both mitosis and interphase, as well as displayed potent anti-proliferative activity (~90% have less than 1μM GI50 value) in the NCI-60 cell line panel compromising nine different cancer types.

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技术信息

生物活性

描述TACC3 (transforming acidic coiled-coil 3), a transforming acidic coiled-coil (TACC) family member, is frequently upregulated in a broad spectrum of cancers, including breast cancer. It plays critical roles in protecting microtubule stability and centrosome integrity that is often dysregulated in cancers. BO-264 is a potential TACC3 inhibitor having an IC₅₀ of 188 nM. Treatment of JIMT-1 cells with 1 μM BO-264 for 6 hours has led to a considerable stabilization of the cellular TACC3 upon increased temperatures. BO-264 inhibited the viability of basal (MDA-MB-231, MDA-MB-436, CAL51, and HCC1143) and HER2+ (JIMT-1 and HCC1954) breast cancer cell lines at lower doses compared with luminal A (MCF-7, T-47D, and ZR-75-1) and luminal B (BT-474) breast cancer cell lines. Similarly, a significantly lower average colony number of JIMT-1 cells was seen upon treatment with BO-264 for 12 days. Despite a relatively lower sensitivity to TACC3 inhibition in RT4 cells, BO-264 yielded the lowest IC₅₀ value in both models (two human urinary bladder cancer cell lines, RT112 and RT4) as compared with SPL-B and KHS101 (other TACC3 inhibitors), suggesting BO-264 might be a highly relevant therapeutic opportunity to target FGFR3–TACC3 fusion-harboring tumors. Moreover, BO-264 decreased ERK1/2 phosphorylation, which is a marker for activated FGFR signaling along with a strong mitotic arrest at minimum 10× lower doses than other TACC3 inhibitors, suggesting that BO-264 specifically blocks the function of FGFR3–TACC3 fusion protein. BO-264 exhibited a remarkable anticancer activity against more than 90% of the cell lines representing nine different subpanels with GI₅₀ values less than 1 μM. siTACC3-induced mitotic arrest, apoptosis, and DNA damage were fully recapitulated by BO-264 in a dose-dependent manner. Furthermore, treatment of JIMT-1 cells with BO-264 for 48 hours induced a prominent increase (from 4.1% to 45.6%) in the fraction of apoptotic cells^[1].
参考文献

[1] Akbulut O, Lengerli D, Saatci O, et al. A Highly Potent TACC3 Inhibitor as a Novel Anticancer Drug Candidate. Mol Cancer Ther. 2020;19(6):1243-1254

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8299 mL
- 14.1493 mL
- 28.2985 mL
- 5 mM
- 0.5660 mL
- 2.8299 mL
- 5.6597 mL
- 10 mM
- 0.2830 mL
- 1.4149 mL
- 2.8299 mL

技术信息

CAS号

2408648-20-2

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19N5O3

运输

蓝冰

分子量

353.38

别名

溶解度

DMSO	71.0 mg/mL (200.9 mM)
Water	Insoluble
Ethanol	Insoluble

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