Uses
AZ304 is potent dual BRAF inhibitor. Is a combination of MEK and B-raf inhibitors for treatment of cancer.
Biological Activity
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.
in vitro
AZ304 inhibited wild-type BRAF and CRAF, BRAF in vitro.
in vivo
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
| 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>
