Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.
产品描述 | MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. |
靶点活性 | MEK2:17 nM , MEK2:9.3 nM (dc50, in SK-MEL-28 cells), MEK1:31 nM (dc50, in HT29 cells), MEK1:31 nM (dc50, in SK-MEL-28 cells) |
体外活性 | a first-in-class degrader of MEK1/2, MS432 (23), which potently and selectively degraded MEK1 and MEK2 in a VHL E3 ligase- and proteasome-dependent manner and suppressed ERK phosphorylation in cells.?It inhibited colorectal cancer and melanoma cell proliferation much more effectively than its negative control MS432N (24), and its effect was phenocopied by MEK1/2 knockdown. |
体内活性 | MS432 (23)Compound 23 was highly selective for MEK1/2 in global proteomic profiling studies.?It was also bioavailable in mice and can be used for in vivo efficacy studies.?We provide two well-characterized chemical tools to the biomedical community. |
分子量 | 1076.06 |
分子式 | C50H65F3IN7O6S |
CAS No. | T13782 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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