Home Protein Tyrosine Kinase VEGFR inhibitor - Raf inhibitor - c-RET inhibitor BAW2881 (NVP-BAW2881) For research use only.

BAW2881 (NVP-BAW2881)

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.

BAW2881 (NVP-BAW2881) Chemical Structure

BAW2881 (NVP-BAW2881) Chemical Structure

CAS No. 861875-60-7

Purity & Quality Control

Batch: S818901 DMSO]84 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.24%
99.24

BAW2881 (NVP-BAW2881) Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

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)		 Click to View More Targets
9 nM 24 nM 76 nM 99 nM 165 nM
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models K14/VEGF-A TG mice
Dosages 25 mg/kg/day
Administration oral administration

Chemical Information & Solubility

Molecular Weight 424.38 Formula

C22H15F3N4O2
CAS No. 861875-60-7 SDF Download BAW2881 (NVP-BAW2881) SDF
Smiles C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC(=NC=C4)N)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (197.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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