Chemical Structure : Belvarafenib
CAS No.: 1446113-23-0
Catalog No.: PC-61364Not For Human Use, Lab Use Only.
Belvarafenib (HM95573, GDC-5573) is a 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, GDC-5573) is a potent, selective RAF inhibitor with IC50 of 41 nM, 7 nM and 2 nM for BRAF WT, BRAF V600E and CRAF, respectively.
Belvarafenib (HM95573, GDC-5573) 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, GDC-5573) 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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