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Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. Refametinib potently inhibited MEK activity as measured by phosphorylation of ERK1/2 across several human cancer cell lines of different tissue origins and BRAF mutational status with EC50 values ranging from 2.5 to 15.8 nM. RDEA119 inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 values ranging from 67 to 89 nM. Refametinib (BAY 86-9766) exhibited potent antiproliferative activity in HCC cell lines with half-maximal inhibitory concentration values ranging from 33 to 762 nM. BAY 86-9766 was strongly synergistic with sorafenib in suppressing tumor cell proliferation and inhibiting phosphorylation of the extracellular signal-regulated kinase (ERK). Refametinib (BAY 869766, RDEA119) exhibits complete suppression of ERK phosphorylation at fully efficacious doses in mice. Refametinib (BAY 869766, RDEA119) shows a tissue selectivity that reduces its potential for central nervous system-related side effects.
| Cell Experiment | |
|---|---|
| Cell lines | A375, SK-MEI-28, Colo205, HT-29 and BxPC3 cells |
| Preparation method | For anchorage-dependent growth inhibition experiments, plating cells in white 384-well plates at 1,000/20 μL/well or white 96-well microplates at 4,000/100 μL/well. After 24-h incubation at 37 °C, 5% CO2, and 100% humidity,incubating RDEA119 for 48 hours at 37 °C and assayed using CellTiter-Glo. For the 96-well anchorage-independent growth assay, filling wells of an “ultralow binding” plate (Corning) are with 60 μL of a 0.15% agarose solution in complete RPMI 1640. Then, adding 60 μL of complete RPMI 1640 which contains 9,000 cells in 0.15% agarose per well. 24 hourlater , adding 60 μL of a 3 × drug solution in agarose-free complete RPMI 1640 . 7 d later , 36 μL of 6 × 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)- 2H-tetrazolium, adding inner salt reagent per well. After 2 hours at 37 °C, determining absorbance at 490 nm on the M5 plate reader. |
| Concentrations | 10-1000 nM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female athymic nude mice are injected s.c. with A375, HT-29 and A431 tumor; male athymic nude mice with Colo205 tumor |
| Formulation | RDEA119 is dissolved in saline. |
| Dosages | 25 or 50 mg/kg |
| Administration | Orally once daily for 14 days |
| Molecular Weight | 572.34 |
| Formula | C19H20F3IN2O5S |
| CAS Number | 923032-37-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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