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 DC 50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
性状
Solid
IC50 & Target[1][2]
MEK1 31 nM (DC50, in HT29 cells) MEK2 17 n
体外研究(In Vitro)
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). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay-tbl">
体内研究(In Vivo)
MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI 50 values of compound 23 in the tested cancer cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 260 mg/mL (241.62 mM; Need ultrasonic)配制储备液