Mechanism of action: B-Raf serine/threonine-protein kinase (BRAF) and V600E mutant inhibitor

Preclinical pharmacology

AZ12823138 binds BRAF and V600E with a potency of 20nM. Cell GI50 proliferation in BRAF MT cell lines is <0.5uM, whereas in BRAF WT cell line have GI50 >20uM.

AZ12823138 showed tumour growth inhibition at 25mpk BID for 10 days in A375 tumour model containing BRAF and V600E. PD (pERK decrease) was confirmed by IHC on tissue collected at 2 hours post last dose.

Additional Information

Gene information from the NCBi

This compound works on the following genes: