MS432 is a highly selective MEK1/2 degrader with IC50=31 nM. MS432 potently and selectively degraded MEK1 and MEK2 in a VHL E3 ligase- and proteasome-dependent manner and suppressed ERK phosphorylation in cells. MS432 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. MS432 potently reduced MEK1/2 protein levels and inhibited ERK signaling, and suppressed cancer cell proliferation effectively. MS432 displayed good plasma exposure in mice and can be used in the in vivo efficacy studies.
MedKoo Cat#: 408052
Name: MS432
CAS#: Unknown
Chemical Formula: C50H65F3IN7O6S
Exact Mass: 1075.3714
Molecular Weight: 1076.07
Elemental Analysis: C, 55.81; H, 6.09; F, 5.30; I, 11.79; N, 9.11; O, 8.92; S, 2.98
The following data is based on the product molecular weight 1,076.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
