AZ304 is potent dual BRAF inhibitor. Is a combination of MEK and B-raf inhibitors for treatment of cancer.
AZ304 is a synthetic inhibitor targeting wild-type and V600E mutant BRAF with IC50 of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R with IC50 below 100 nM.
AZ304 inhibited wild-type BRAF and CRAF, BRAF in vitro.
In both RKO and Caco-2 tumor models, administration of AZ304 alone or in combination with Cetuximab resulted in antitumor activity without apparent toxic effects (regardless of BRAF mutation).
| Target | Value |
p38
(Cell-free assay) | 6 nM |
CSF1R
(Cell-free assay) | 35 nM |
< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BRAF(V600E)
(Cell-free assay) 38 nM |
CRAF
(Cell-free assay ) | 68 nM |
WT BRAF
(Cell-free assay) | 79 nM | < /tr>
BRafV600E: 38 nM (IC50); BRAFWT: 79 nM (IC50); CRAF: 68 nM (IC50); p38: 6 nM (IC50); CSF1R: 35 nM (IC50); MAP3K7: 6400 nM (IC50); CSK: 7050 nM (IC50)
