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MS432
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MS432图片
规格:98%
分子量:1076.06
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
MS432 是创新的、高度选择性的、基于 PD0325901 和 von Hippel-Lindau 配体的 MEK1 和 MEK2 的 PROTAC 降解剂。MS432 在小鼠体内显示了较高且长时间的血浆暴露量,对 HT29 细胞中 MEK1 和 MEK2 蛋白的DC50 值分别为 31 nM 和 17 nM。
货号:ajcx37332
CAS:2672512-44-4
分子式:C50H65F3IN7O6S
分子量:1076.06
溶解度:DMSO : 260 mg/mL (241.62 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively[1].

MS432 (compound 23) is potent in reducing MEK1/2 protein levels in COLO 205 cells (DC50 (MEK1) = 18 ± 7 nM, DC50 (MEK2) = 11 ± 2 nM) and UACC257 cells (DC50 (MEK1) = 56 ± 25 nM, DC50 (MEK2) = 27 ± 19 nM).

MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI50 values of compound 23 in the tested cancer cell lines[1].

[1]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911.