BGB-283
- Lifirafenib
- Optical Purity: 0.99
- Soluble in DMSO
- MF: C25H17F3N4O3
- MW: 478.42
Description
BGB-283 is an orally available dual RAF kinase/EGFR inhibitor. It potently inhibits BRAF family proteins (wild-type ARAF, BRAF, CRAF and BRAF V600E), BRAF(V600E)-activated ERK phosphorylation and cell proliferation, and demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAF(V600E) and EGFR mutation/amplification. Further, it uniquely displays inhibitory activity towards both BRAF monomeric and dimeric forms, and is considered to be the next generation inhibitor to potentially address resistances associated with increased BRAF dimer formation in response to treatment with first-generation BRAF inhibitors.
More Information
| Parent CAS No. | 1446090-77-2 |
|---|---|
| Chemical Name | rel-5-[[(1S,1aS,6bR)-1a,6b-dihydro-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1H-cyclopropa[b]benzofuran-5-yl]oxy]-3,4-dihydro1,8-Naphthyridin-2(1H)-one |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(OC2C=CN=C3NC(=O)CCC=23)C=C2[C@H]3[C@H](C4=NC5C=CC(C(F)(F)F)=CC=5N4)[C@H]3OC2=CC=1 |&1:15,16,30,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1 |
| InChiKey | NGFFVZQXSRKHBM-FKBYEOEOSA-N |
| CID | 89670174 |
| Short Description | RAF kinase and EGFR inhibitor |
References
- Z Tang et al. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.
- CC Li et al. Small molecule RAF265 as an antiviral therapy acts against HSV-1 by regulating cytoskeleton rearrangement and cellular translation machinery. J Med Virol. 2023 Jan;95(1):e28226.
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