VEGFR

Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.

BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.

TG 100801 is a VEGFR2 targeting prodrug currently in a clinical trial. The active form is TG100572.

TG 100572 is VEGFR2 and Src kinase inhibitor.

N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively).

TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.

TG 100801 is the prodrug of TG 100572 (HY-10184), TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.

SU10944 is a small molecule kinase inhibitor of VEGFR that inhibits neovascularization and permeability, and is distributed to the eye upon systemic delivery.

Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor.

VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.

BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.

Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.