Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VU0661013 是一种有效的选择性 MCL-1 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,790 | 现货 | ||
5 mg | ¥ 4,420 | 现货 | ||
10 mg | ¥ 6,280 | 现货 | ||
25 mg | ¥ 9,520 | 现货 | ||
50 mg | ¥ 12,800 | 现货 | ||
100 mg | ¥ 17,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,560 | 现货 |
产品描述 | VU0661013 is an effective and selective inhibitor of MCL-1. |
体外活性 | VU0661013 does not obviously suppress BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM). VU0661013 shows a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK [1]. |
体内活性 | VU0661013 is a potent and selective MCL-1 inhibitor and is active in Venetoclax-resistant cells and patient-derived xenografts. VU0661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU0661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amending spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU0661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days) [1]. |
别名 | VU661013 |
分子量 | 712.66 |
分子式 | C39H39Cl2N5O4 |
CAS No. | 2131184-57-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 117mg/mL (164.2mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4032 mL | 7.016 mL | 14.0319 mL | 35.0798 mL |
5 mM | 0.2806 mL | 1.4032 mL | 2.8064 mL | 7.016 mL | |
10 mM | 0.1403 mL | 0.7016 mL | 1.4032 mL | 3.508 mL | |
20 mM | 0.0702 mL | 0.3508 mL | 0.7016 mL | 1.754 mL | |
50 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7016 mL | |
100 mM | 0.014 mL | 0.0702 mL | 0.1403 mL | 0.3508 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。
VU0661013 2131184-57-9 Apoptosis BCL VU 661013 VU 0661013 VU661013 VU-661013 VU-0661013 Inhibitor inhibitor inhibit