| Chemical Properties | Back Directory | [density ]
1.354±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, protect from light, stored under nitrogen | [solubility ]
DMSO : 260 mg/mL (241.62 mM; Need ultrasonic) | [form ]
Solid | [pka]
13.97±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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. |
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