BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
Product Description
Information
BFH772 is a novel potent oralVEGFR2inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
Targets
VEGFR2 (Cell-free assay) 3 nM
In vitro
BFH772 was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.
In vivo
BFH772 all at 3 mg/kg orally dosed once per day potently inhibited melanoma growth (by 54−90% for primary tumor and 71−96% for metastasis growth).
