BFH772

Catalog No.S8188 Synonyms: BFH 772, BFH-772

BFH772 Chemical Structure

Molecular Weight(MW): 439.39

BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.

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Biological Activity

Description BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
Targets
VEGFR2 [1]
(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[1].

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)[1].

Protocol

Cell Research:[1]
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  • Cell lines: HUVEC endothelial cells
  • Concentrations: 0-10 nM
  • Incubation Time: 48 h
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Sprague−Dawley rats
  • Formulation: N-methyl pyrrolidone/polyethylene glycol200(30:70, v/v)
  • Dosages: 1 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (198.0 mM)
Ethanol 87 mg/mL (198.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 439.39
Formula

C23H16F3N3O3

CAS No. 890128-81-1
Storage powder
Synonyms BFH 772, BFH-772

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID