Chemical Structure : Belvarafenib
CAS No.: 1446113-23-0
Catalog No.: PC-61364Not For Human Use, Lab Use Only.
Belvarafenib (HM95573, GDC5573) is a novel potent, selective RAF inhibitor with IC50 of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF V600E and CRAF, respectively.
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Belvarafenib (HM95573, GDC5573) is a novel potent, selective RAF inhibitor with IC50 of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF V600E and CRAF, respectively.
Belvarafenib (HM95573, GDC5573) inhibits cell proliferation of A375 (BRAF V600E) and SK-MEL-30 (NRAS Q61K) with IC50 of 57 and 24 nM, also inhibits the phosphorylations of MEK and ERK downstream kinases in mutant BRAF and mutant NRAS melanoma cells.
Belvarafenib (HM95573, GDC5573) shows the excellent antitumor activity in mouse models xenografted with both of BRAF mutation cell lines (e.g. A375 and SK-MEL-28) and NRAS mutation cell lines.
M.Wt | 478.93 | |
Formula | C23H16ClFN6OS | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide |
1. InHwan Bae, et al. Antitumor activity of the selective RAF inhibitor HM95573 in melanoma. AACR 2015. DOI: 10.1158/1538-7445.AM2015-2606
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