Regorafenib (BAY 73-4506) mesylate is an orally active multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1/2/3 (IC50=13/4.2/46 nM), PDGFRβ (IC50: 22 nM), Kit (IC50: 7 nM), RET (IC50: 1.5 nM) and Raf-1 (IC50: 2.5 nM). Regorafenib mesylate has potent anti-tumour and anti-angiogenic effects.

VEGFR3:46 ± 10 nM, B-Raf (V600E):19 ± 6 nM, VEGFR1:13 ± 0.4 nM, B-Raf:28 ± 10 nM, VEGFR2:4.2 ± 1.6 nM, Tie2:311 ± 46 nM, PDGFRβ:22 ± 3 nM, Raf-1:2.5 ± 0.6 nM