Regorafenib: A Multikinase Inhibitor of Tumour Angiogenesis, Oncogenesis and the Tumour Microenvironment
Regorafenib (BAY 73-4506) is a potent diphenylurea multikinase inhibitor of tumour angiogenesis (VEGFR1,VEGFR2,VEGFR3,TIE2), oncogenesis (KIT, RET, RAF-1, BRAF, BRAF
V600E), and the tumour microenvironment (PDGFR-β, FGFR). Regorafenib has promising antineoplastic activity in various tumor types. Regorafenib is mainly metabolized by CYP3A4, and the major human metabolites M-2 (
N-oxide) and M-5 (
N-oxide and
N-desmethyl) are reported to exhibited similar efficacies compared to regorafenib in
in vitro and
in vivo models. For your reference, [
A2979] is a key synthetic intermediate of regorafenib. (The product is for research purpose only.)