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BFH772

Catalog No. T3599 CAS 890128-81-1

Synonyms: BFH-722

BFH772, a structure analogue of BAW2881, is a potent and selective VEGF inhibitor. BFH772 is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.

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BFH772, CAS 890128-81-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 60.00
10 mg	In stock	$ 105.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 297.00
100 mg	In stock	$ 563.00
1 mL * 10 mM (in DMSO)	In stock	$ 67.00

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Purity: 99.36%

Purity: 97.71%

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Description	BFH772, a structure analogue of BAW2881, is a potent and selective VEGF inhibitor. BFH772 is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.
Targets&IC50	VEGFR2:3 nM
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%.
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.
Kinase Assay	In vitro kinase assay is based on a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-sepharose, γ-[33P]ATP as the phosphate donor, and poly(Glu:Tyr 4:1) peptide as the acceptor. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1-3 mM MnCl2, 3-10 mM MgCl2, 3-8 μg/mL poly(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT] and 0.2 μCi γ-33P ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 min at ambient temperature. The reaction is stopped by adding 10 mL of 250 mM EDTA. Using a 384-well filter system, half the volume is transferred onto an Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively and dried, and scintillation counting is performed. IC50s for compounds are calculated by linear regression analysis of the percentage inhibition[1].
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)

Synonyms	BFH-722
Molecular Weight	439.39
Formula	C23H16F3N3O3
CAS No.	890128-81-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 81 mg/mL (184.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 81 mg/mL (184.3 mM)

References and Literature

1. Bold G, et al. J Med Chem. 2016, 59(1):132-46.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Kinase Inhibitor Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Prostate Cancer Compound Library Anti-Lung Cancer Compound Library

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Keywords

BFH772 890128-81-1 Angiogenesis Tyrosine Kinase/Adaptors VEGFR BFH-772 inhibit BFH-722 BFH 722 Vascular endothelial growth factor receptor Inhibitor BFH722 BFH 772 inhibitor

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