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Background Information:
BGB-283 (Lifirafenib) 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.
Reference:
1. 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. doi: 10.1158/1535-7163.MCT-15-0262. Epub 2015 Jul 24.
APIM050023: BGB-283 (Lifirafenib)
CAS No.: 1446090-77-2.
Molecular Formula: C25H17F3N4O3?1.3H2O.
Molecular Weight: 501.8.
Purity: >99.5% chem and optical purity by achiral and chiral HPLCs.
QC: HPLC-MS, 1H-NMR, Chiral HPLC, and Elemental Analysis Report.
Solubility: Refer to Certificate.
Storage: Refer to Certificate.
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