Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 5,410 | 待询 | ||
10 mg | ¥ 7,890 | 待询 | ||
25 mg | ¥ 16,200 | 待询 | ||
50 mg | ¥ 24,500 | 待询 | ||
100 mg | 待询 | 待询 | ||
200 mg | 待询 | 待询 |
产品描述 | BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity. |
体外活性 | BETd-246 treatment (0-100 nM, 1-3 h) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation. BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines[1]. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated and it also induces much stronger apoptosis than BETi-211. |
体内活性 | BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models[1]. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. |
分子量 | 946.02 |
分子式 | C48H55N11O10 |
CAS No. | 2140289-17-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (211.41 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 | 1.0571 mL | 5.2853 mL | 10.5706 mL | 26.4265 mL |
5 mM | 0.2114 mL | 1.0571 mL | 2.1141 mL | 5.2853 mL | |
10 mM | 0.1057 mL | 0.5285 mL | 1.0571 mL | 2.6427 mL | |
20 mM | 0.0529 mL | 0.2643 mL | 0.5285 mL | 1.3213 mL | |
50 mM | 0.0211 mL | 0.1057 mL | 0.2114 mL | 0.5285 mL | |
100 mM | 0.0106 mL | 0.0529 mL | 0.1057 mL | 0.2643 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。
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