Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 1,990 | 现货 | ||
50 mg | ¥ 2,970 | 现货 | ||
100 mg | ¥ 4,280 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3, IC50 of 188 nM and a Kd of 1.5 nM). |
靶点活性 | TACC3:188 nM (IC50), TACC3:1.5 nM (Kd) |
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. |
分子量 | 353.38 |
分子式 | C18H19N5O3 |
CAS No. | 2408648-20-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (141.49 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8298 mL | 14.1491 mL | 28.2981 mL | 70.7454 mL |
5 mM | 0.566 mL | 2.8298 mL | 5.6596 mL | 14.1491 mL | |
10 mM | 0.283 mL | 1.4149 mL | 2.8298 mL | 7.0745 mL | |
20 mM | 0.1415 mL | 0.7075 mL | 1.4149 mL | 3.5373 mL | |
50 mM | 0.0566 mL | 0.283 mL | 0.566 mL | 1.4149 mL | |
100 mM | 0.0283 mL | 0.1415 mL | 0.283 mL | 0.7075 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
BO-264 2408648-20-2 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR inhibit cytotoxicity antitumor Fibroblast growth factor receptor Inhibitor TACC3 spindle abnormalities ERK1/2 DNA phosphorylation BO 264 FGFR3-TACC3 mitotic damage anti-proliferative BO264 inhibitor