BFH772

SKU: orb1304013

Description

BFH772 is a potent and selective small-molecule VEGF inhibitor, structurally analogous to BAW2881. It primarily targets VEGFR2 kinase with high potency (IC50 = 3 nM) and also inhibits RET, PDGFR, and KIT autophosphorylation. This profile supports its research use in angiogenesis, oncology, and related in vitro and in vivo studies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 890128-81-1
• MW: 439.39
• Purity: 99.89%
• Formula: C₂₃H₁₆F₃N₃O₃
• SMILES: OCc1cc(Oc2ccc3c(cccc3c2)C(=O)Nc2cccc(c2)C(F)(F)F)ncn1
• Target: VEGFR
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (7.51 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:81 mg/mL (184.35 mM);DMSO:81 mg/mL (184.35 mM)

Bioactivity

• Target IC50:
  VEGFR2:3 nM
• In Vivo:
  BFH772 inhibits ligand-induced autophosphorylation of RET, PDGFR, and KIT kinases with an IC50 (half maximal inhibitory concentration) value of 30-160 nM. It effectively targets VEGFR2 with an IC50 of 3 nM, demonstrating efficacy 500 times lower against FLK-1, FLT-1, and FLT-4 compared to VEGFR2. Beyond VEGFR2, BFH772 also targets B-RAF, RET, and TIE-2, albeit with over 40 times lower efficacy compared to its action on VEGFR2.
• In Vitro:
  Daily oral administration of 3 mg/kg BFH772 effectively inhibits melanoma growth, with primary tumors reducing by 54-90% and metastatic tumors diminishing by 71-96%.
• Cell Research:
  Subconfluent HUVECs were incubated in triplicate in 96-well plates with basal medium containing 1.5% FCS and a constant concentration of VEGF (10 ng/mL), bFGF (0.5 ng/mL), or FCS (5%) in the presence or absence of compounds. After 24 h of incubation, BrdUrd labeling solution was added and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidaselabeled anti-BrdUrd antibody. Bound antibody was then detected spectrophotometrically at 450 nm.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BFH 722, BFH 772, BFH722, BFH-722, BFH772, BFH-772, Inhibitor, inhibit, VEGFR2, VEGFR, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

24756034