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RO5126766 (CH5126766, VS 6766) is a first-in-class dual MEK/RAF inhibitor with IC50 values of 8.2 nM, 19 nM, 56 nM and 160 nM for BRAF V600E, BRAF, CRAF and MEK1, respectively. In HCT116 KRAS-mutant colorectal cancer cells, CH5126766 significantly reduces the levels of phospho-MEK and phospho-ERK. CH5126766 inhibits RAF kinase by binding to MEK1, and causes MEK to become a dominant negative inhibitor of RAF. In Raf or RAS-mutant cell lines SK-MEL-28, SK-MEL-2, MIAPaCa-2, SW480, HCT116, and PC3 cells, CH5126766 inhibits cell growth with IC50 of 65, 28, 40, 46, and 277 nM, respectively.
In vivo, RO5126766 (25 mg/kg, p.o.) inhibits ERK signaling output more effectively in an HCT116 (G13D KRAS) mouse xenograft model than a standard MEK inhibitor that induces MEK phosphorylation, and has potent antitumor activity. In the HCT116 (K-ras) and COLO205 (B-raf) mutant xenografts, CH5126766 (0.3 mg/kg) causes significant decreases in [18F]FDG uptake.
| Molecular Weight | 471.46 |
| Formula | C21H18FN5O5S |
| CAS Number | 946128-88-7 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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