RAF265
RAF265 is an orally bioavailable anticancer chemotherapeutic compound that inhibits primarily WT B-Raf, mutant (V600E) B-Raf, and VEGFR2, but is also active against c-Raf, PDGFR, CSF-1R, RET, c-Kit, Src, and STE20. This compound is in clinical trials as a treatment for unresectable or metastatic melanoma. Inhibition of B-Raf by RAF265 attenuates downstream ERK and RET signaling, preventing tumor cell proliferation. Raf265-induced alterations in ERK signaling also decreases expression of c-fos and NFATc1, inhibiting in vitro differentiation of PBMCs to osteoclasts and inhibiting osteoclast resorptive capacity, therefore inhibiting osteoclastogenesis.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18957353
| Cas No. |
927880-90-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H16F6N6O |
| Formula Wt. |
518.4 |
| Chemical Name |
1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine |
| IUPAC Name |
CN1C2=C(C=C(C=C2)OC3=CC(=NC=C3)C4=NC=C(N4)C(F)(F)F)N=C1NC5=CC=C(C=C5)C(F)(F)F |
| Solubility |
DMSO 100 mg/mL |
Garcia-Gomez A, Ocio EM, Pandiella A, et al. RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications. Invest New Drugs. 2013 Feb;31(1):200-5. d PMID: 22773056.
Huang T, Karsy M, Zhuge J, et al. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. PMID: 23617957.
Su Y, Vilgelm AE, Kelley MC, et al. RAF265 inhibits the growth of advanced human melanoma tumors. Clin Cancer Res. 2012 Apr 15;18(8):2184-98. Erratum in: Clin Cancer Res. 2012 Aug 15;18(16):4475. PMID: 22351689.
