Cat. No.: HY-100419

BFH772

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Based on 1 Customer Validation

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC₅₀ value of 3 nM.

For research use only. We do not sell to patients.

Purity: 96.67%
CAS No.: 890128-81-1
Formula: C₂₃H₁₆F₃N₃O₃
Molecular Weight:439.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BFH772 Chemical Structure

CAS No.: 890128-81-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC₅₀ value of 3 nM^[1].

IC₅₀ & Target^[1]

VEGFR2

3 nM (IC₅₀)

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	>10 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	0.002 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	0.027 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	0.104 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	6.54 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	7.2 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
BaF3	IC₅₀	7.5 μM Compound: BFH772	Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay	[PMID: 26629594]
HUVEC	IC₅₀	<0.01 nM Compound: BFH772	Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis	[PMID: 26629594]
HUVEC	IC₅₀	>3 μM Compound: BFH772	Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis	[PMID: 26629594]

In Vitro

BFH772 is highly selective; apart from inhibiting VEGFR2 at 3 nM IC₅₀, it also targets B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 is inactive (IC₅₀>10 μM; >2 μM for cKIT) against all other tyrosine specific- and serine/threonine-specific protein kinases tested. BFH772 inhibits VEGFR2 with IC₅₀ of 4.6±0.6 nM in CHO cells. BFH772 inhibits VEGFR2 with IC₅₀ of 3 nM in HUVEC cells. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC₅₀ values ranging between 30 and 160 nM. BFH772 is selective (IC₅₀ values >0.5 μM) against the kinases of EGFR, ERBB2, INS-R, and IGF-1R and against the cytoplasmic BCR-ABL kinase. IC₅₀ of BFH772 (<0.01 nM, n=2) demonstrates that they abrogated VEGF induced proliferation at remarkably low nM concentrations^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BFH772 at 3 mg/kg orally dosed once per day potently inhibits melanoma growth (by 54-90% for primary tumor and 71-96% for metastasis growth) as depicted by treatment to control ratios. Dose–response curves of BFH772 at 0.3, 1, and 3 mg/kg demonstrate that even at the lowest concentrations, this naphthalene-1-carboxamide inhibits VEGF induced tissue weight and TIE-2 levels but only reaches statistical significance at 1 mg/kg and above^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 890128-81-1
Appearance Solid
Molecular Weight 439.39
Formula C₂₃H₁₆F₃N₃O₃
Color White to off-white
SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1)C2=CC=CC3=CC(OC4=NC=NC(CO)=C4)=CC=C32
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (227.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2759 mL

11.3794 mL

22.7588 mL

5 mM

0.4552 mL

2.2759 mL

4.5518 mL

10 mM

0.2276 mL

1.1379 mL

2.2759 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[1]

Different Ba/F3 cell lines rendered IL-3 independent by transduction with various constitutively active tyrosine kinases are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental Ba/F3 cells, the medium is additionally supplemented with 10 ng/mL interleukin-3 (IL-3). For proliferation assays, Ba/F3 cells are seeded on 96-well plates in triplicates at 10000 cells per well and incubated with various concentrations of compounds for 72 h followed by quantification of viable cells using a resazurin sodium salt dye reduction readout (commercially known as Alamar Blue assay). IC₅₀s are determined with the XLFit Excel Add-In using a four-parameter dose response model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Female FVB mice weighing between 18 and 20 g are housed in groups of six. Porous chambers containing VEGF (2 μg/mL) in 0.5 mL of 0.8% w/v agar (containing heparin, 20 U/mL) are implanted subcutaneously in the flank of the mice (n=6 per group). VEGF induces the growth of vascularized tissue around the chamber. This response is dose-dependent and can be quantified by measuring the weight and TIE-2 levels of the tissue. Mice are treated either orally once daily with compounds or vehicle (PEG200 100%, 5 mL/kg) starting 4-6 h before implantation of the chambers and continuing for 4 days. The animals are sacrificed for measurement of the vascularized tissues 24 h after the last dose. Tissue weight is taken and then a lysate prepared for TIE-2 ELISA analysis .
Rats^[1]
Catheters are implanted into the femoral artery and vein of naïve female rats strain OFA for BFH772, and BAW2881, or in the jugular vein and femoral artery in female Sprague-Dawley rats for compounds 4, 9, and 10. Animals are allowed to recover for 96 h and are housed in single cages with free access to food and water throughout the experiment. Female OFA rats received 2.5 mg/kg of BAW2881 dissolved in ethanol/dimethylisosorbide/polyethylene glycol400/D5W (10/15/35/40 v/v) or 1 mg/kg of BFH772 dissolved in N-methyl pyrrolidone/polyethylene glycol200 (30:70, v/v) via injection into the femoral vein. D5W is glucose 5%/water (v/v). Oral administration: BAW2881 and BFH772 are formulated as a micronized suspension (dissolved/suspended in 0.5% carboxymethyl cellulose in distilled water) and administered by gavage to female OFA rats to deliver a dose of 25 mg/kg for BAW2881 or 3 mg/kg BFH772 (n=4 rats per group). For compounds 4, 9, and 10, female Sprague-Dawley rats at 8 weeks of age received an intravenous dose of 3 mg/kg 4, 9, and 10, formulated in ethanol/NMP/polyethylene glycol400/D5W (10/10/50/30) (n=2 rats per group), or a suspension in 0.5% carboxymethyl cellulose in distilled water dosed at 50 mg/kg (n=3 rats per group). At the allotted times, blood samples are collected into heparinized tubes, and the amount of compound in plasma determined by HPLC/MS-MS.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bold G, et al. A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis. J Med Chem. 2016 Jan 14;59(1):132-46. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2759 mL	11.3794 mL	22.7588 mL	56.8971 mL
	5 mM	0.4552 mL	2.2759 mL	4.5518 mL	11.3794 mL
	10 mM	0.2276 mL	1.1379 mL	2.2759 mL	5.6897 mL
	15 mM	0.1517 mL	0.7586 mL	1.5173 mL	3.7931 mL
	20 mM	0.1138 mL	0.5690 mL	1.1379 mL	2.8449 mL
	25 mM	0.0910 mL	0.4552 mL	0.9104 mL	2.2759 mL
	30 mM	0.0759 mL	0.3793 mL	0.7586 mL	1.8966 mL
	40 mM	0.0569 mL	0.2845 mL	0.5690 mL	1.4224 mL
	50 mM	0.0455 mL	0.2276 mL	0.4552 mL	1.1379 mL
	60 mM	0.0379 mL	0.1897 mL	0.3793 mL	0.9483 mL
	80 mM	0.0284 mL	0.1422 mL	0.2845 mL	0.7112 mL
	100 mM	0.0228 mL	0.1138 mL	0.2276 mL	0.5690 mL

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BFH772

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-COVID-19 Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All VEGFR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

BFH772 Related Classifications

HY-100419 Related Classifications