| 产品描述： | TACC3 抑制剂;TACC3 Inhibitors;;InformationBO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.TargetsFGFR3 ; TACC3 (Cell-free assay); TACC3 (Cell-free assay) ; 1.5 nM(Kd); 188 nMIn vitroBO-264 significantly decreases centrosomal TACC3 during both mitosis and interphase. BO-264 displays potent anti-proliferative activity in the NCI- 60 cell line panel compromising nine different cancer types. BO-264 significantly inhibits the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.In vivoBO-264\'s oral administration significantly impairs tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increases survival without any major toxicity.Cell Research(from reference)Cell lines：JIMT-1 cells Concentrations：1 μM Incubation Time：6 h |
| 靶点： |
IC50: 188 nM (Transforming acidic coiled-coil 3 (TACC3));Kd: 1.5 nM (TACC3) |
| 体内研究： |
BO-264 (25 mg/kg；口服；每天；持续 3-4 周；雌性裸鼠) 处理显示出对肿瘤生长的显著抑制。BO-264 具有良好的耐受性，因为处理不会导致显著的体重减轻和器官毒性。 |
| 参考文献： |
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. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.83 ml |
14.149 ml |
28.298 ml |
| 5 mM |
0.566 ml |
2.83 ml |
5.66 ml |
| 10 mM |
0.283 ml |
1.415 ml |
2.83 ml |
| 50 mM |
0.057 ml |
0.283 ml |
0.566 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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危险品化学品经营许可证（不带存储）
营业执照(三证合一)
