Home Angiogenesis VEGFR inhibitor BFH772 For research use only.

BFH772

Synonyms: BFH 772, BFH-772

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

BFH772 Chemical Structure

BFH772 Chemical Structure

CAS No. 890128-81-1

Purity & Quality Control

Batch: S818801 DMSO]87 mg/mL]false]Ethanol]87 mg/mL]false]Water]Insoluble]false Purity: 99.09%
99.09

BFH772 Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Sprague−Dawley rats
Dosages 1 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00987870 Completed
Psoriasis|Arthritis
Novartis Pharmaceuticals|Novartis
 September 2009 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 439.39 Formula

C23H16F3N3O3
CAS No. 890128-81-1 SDF Download BFH772 SDF
Smiles C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC=NC(=C4)CO)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 87 mg/mL ( (198.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

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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