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BFH772 VEGFR inhibitor

Cat.No.S8188

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

Chemical Structure

Molecular Weight: 439.39

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 439.39 Formula

C23H16F3N3O3

 Storage (From the date of receipt)
CAS No. 890128-81-1 Download SDF Storage of Stock Solutions

Synonyms BFH 772, BFH-772 Smiles C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC=NC(=C4)CO)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (198.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 87 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
VEGFR2 [1]
(Cell-free assay)
3 nM
In vitro
This compound 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. It was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. This chemical 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].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00987870 Completed
Psoriasis|Arthritis
Novartis Pharmaceuticals|Novartis
 September 2009 Phase 1|Phase 2

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