BAW2881 (NVP-BAW2881)

Catalog No.S8189 Batch:S818901

Technical Data

Formula	C₂₂H₁₅F₃N₄O₂
Molecular Weight	424.38	CAS No.	861875-60-7
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (197.93 mM)
		Ethanol	20 mg/mL (47.12 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

BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.

Targets

hVEGFR2 ^[1] (Cell-free assay)	C-Raf-1 ^[1] (Cell-free assay)	B-RAFV599E ^[1] (Cell-free assay)	c-Abl ^[1] (Cell-free assay)	mVEGF2 ^[1] (Cell-free assay)	View More
9 nM	24 nM	76 nM	99 nM	165 nM	View More

In vitro

In vitro studies demonstrated that NVP-BAW2881 inhibited proliferation, migration, and tube formation of human umbilical vein endothelial cells and lymphatic endothelial cells^[2].

In vivo

NVP-BAW2881 targets the tyrosine kinase domain of murine, porcine, and human VEGFR2. It can be administered both orally and topically, but has not been tested in humans. In vivo studies in VEGF-A transgenic mice showed that oral and topical administration of NVP-BAW2881 strongly reduced psoriasis-like inflammation in ear skin. Histologically, skin lesions in treated mice showed reduced infiltration by leukocytes, reduced epidermal hyperproliferation, normalization of epidermal keratinocyte differentiation, and fewer vascular abnormalities. Vessels in treated mice were smaller in size and fewer in number. In comparison to control mice, treated mice showed significant improvement in ear swelling, skin inflammation, lymph node enlargement, and skin erythema. Though both modes of administration were effective, systemic administration of NVP-BAW2881 was more potent than topical administration. Topical NVP-BAW2881 also effectively reduced VEGF-A-induced vascular permeability in the skin of mice and domestic pigs^[2].

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines Human dermal lymphatic endothelial cells(LECs), human umbilical vein endothelial cells(HUVECs) Concentrations 1 nmol/L to 1 mol/L Incubation Time 72 h Method HUVECs or LECs (1.2×10³) were seeded into fibronectin-coated 96-well plates. After 24 hours, the cells were transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells(eight wells/condition) were incubated with medium alone(control), 20 ng/ml VEGF-A, or a combination of 20 ng/ml VEGF-A and 1 nmol/L to 1 mol/L NVP-BAW2881. Proliferation was also assayed in LECs incubated with 500 ng/ml VEGF-C. The dimethyl sulfoxide concentration was adjusted to 0.1% in all wells. After 72 hours, cells were incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a SpectraMax Gemini electron microscope.
Animal Study:^{^[3]}	Animal Models K14/VEGF-A TG mice Dosages 25 mg/kg/day Administration oral administration

Cell Assay:^{^[3]}

Cell lines
Human dermal lymphatic endothelial cells(LECs), human umbilical vein endothelial cells(HUVECs)
Concentrations
1 nmol/L to 1 mol/L
Incubation Time
72 h
Method
HUVECs or LECs (1.2×10³) were seeded into fibronectin-coated 96-well plates. After 24 hours, the cells were transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells(eight wells/condition) were incubated with medium alone(control), 20 ng/ml VEGF-A, or a combination of 20 ng/ml VEGF-A and 1 nmol/L to 1 mol/L NVP-BAW2881. Proliferation was also assayed in LECs incubated with 500 ng/ml VEGF-C. The dimethyl sulfoxide concentration was adjusted to 0.1% in all wells. After 72 hours, cells were incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a SpectraMax Gemini electron microscope.

Animal Study:^{^[3]}

Animal Models
K14/VEGF-A TG mice
Dosages
25 mg/kg/day
Administration
oral administration

References

Selleck's BAW2881 (NVP-BAW2881) has been cited by 2 publications

VEGF-A165 gene therapy ameliorates blood-labyrinth barrier breakdown and hearing loss [ JCI Insight, 2021, 143285]	PubMed: 33690221
Knockdown GREM1 suppresses cell growth, angiogenesis, and epithelial-mesenchymal transition in colon cancer [ J Cell Biochem, 2019, 120(4):5583-5596]	PubMed: 30426548

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SHIPPING AND STORAGE
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