AZ628 is a quinazolinone-based pan-Raf kinase inhibitor with IC50 values of 105, 34, and 29 nM for b-Raf, bRafV600E, and c-Raf-1, respectively. [1] It is selective over a wide panel of RTKs, including VEGFR2, DDR2, Lyn, Flt1, and FMS. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines with the b-RafV600E mutation. Cross-reactivity profiles of AZ628 indicate similarities to sorafenib.

Typically AZ628-sensitive lines are often characterized by b-RAFV600E or NRAS mutations, while HRAS or KRAS mutations were not normally observed. AZ628 sensitivity is correlates with its abaility to suppress downstream ERK. [2]

AZ628 is a quinazolinone-based pan-Raf kinase inhibitor with IC50 values of 105, 34, and 29 nM for b-Raf, bRafV600E, and c-Raf-1, respectively. [1] It is selective over a wide panel of RTKs, including VEGFR2, DDR2, Lyn, Flt1, and FMS. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines with the b-RafV600E mutation. Cross-reactivity profiles of AZ628 indicate similarities to sorafenib.

Typically AZ628-sensitive lines are often characterized by b-RAFV600E or NRAS mutations, while HRAS or KRAS mutations were not normally observed. AZ628 sensitivity is correlates with its abaility to suppress downstream ERK. [2]