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Background Information:
Belvarafenib (GDC5573, HM95573, RG6185) is a potent and selective Type II pan-RAF inhibitor with IC50s of 41 nM, 7 nM and 2 nM for BRAF (WT), B-RAF (V600E) and C-RAF, respectively; inhibits cell proliferation of A375 (BRAF V600E) and SK-MEL-30 (NRAS Q61K) with IC50s of 57 and 24 nM, respectively; It also inhibits the phosphorylations of MEK and ERK downstream kinases in mutant BRAF and mutant NRAS melanoma cells; shows excellent antitumor activities in mouse models xenografted with both of BRAF mutation cell lines (e.g. A375 and SK-MEL-28) and NRAS mutation cell lines.
Reference:
1. T. W. Kim, et al, Belvarafenib, a novel pan-RAF inhibitor, in solid tumor patients harboring BRAF, KRAS, or NRAS mutations: Phase I study, Journal of Clinical Oncology, 37, No. 15_suppl (May 20 2019) 3000-3000.
APIM050022: Belvarafenib (GDC5573, HM95573, RG6185)
CAS No.: 1446113-23-0.
Molecular Formula: C23H16ClFN6OS • 0.4H2O.
Molecular Weight: 486.1.
Purity: >99% by HPLC.
QC: HPLC-MS, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to the Certificate of Analysis.
Storage: Refer to the Certificate of Analysis.
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