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PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAFV600E in mutant RAS expressing cells. PLX7904 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells.
In vivo, PLX7904 inhibits the COLO205 xenograft growth in eight mice per group.
| Cell Experiment | |
|---|---|
| Cell lines | WM793, WM115, WM9, WM278, WM1346, WM1366, WM1361A, Sbcl2, 1205Lu, A375, SK-MEL 24, SKMEL-2, and SK-MEL 207 cells |
| Preparation method | Cells are treated with PLX7904 at different concentrations (0, 0.05, 0.1, 1, 5 μM) for 24 h. Cells are lysed and analyzed by Western blotting with phospho-MEK1/2, total MEK1/2, phospho-ERK1/2 and total ERK1/2 antibodies. |
| Concentrations | 0, 0.05, 0.1, 1, 5 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 512.53 |
| Formula | C24H22F2N6O3S |
| CAS Number | 1393465-84-3 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Zhang C, et al. Nature. RAF inhibitors that evade paradoxical MAPK pathway activation.
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