BFH772

Catalog No.S8188 Batch:S818801

Technical Data

Formula	C₂₃H₁₆F₃N₃O₃
Molecular Weight	439.39	CAS No.	890128-81-1
Solubility (25°C)*	In vitro	DMSO	87 mg/mL (198.0 mM)
		Ethanol	87 mg/mL (198.0 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Sprague−Dawley rats Dosages 1 mg/kg Administration i.v.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Sprague−Dawley rats
Dosages
1 mg/kg
Administration
i.v.

References

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

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SHIPPING AND STORAGE
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