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Belvarafenib

Chemical Structure : Belvarafenib

CAS No.: 1446113-23-0

Belvarafenib (HM95573, GDC-5573, RG6185)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 478.93
Formula C23H16ClFN6OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-amino-N-[1-(3-chloro-2-fluoroanilino)-6-methylisoquinolin-5-yl]thieno[3,2-d]pyrimidine-7-carboxamide

References

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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