Home Protein Tyrosine Kinase VEGFR inhibitor BAW2881 (NVP-BAW2881)

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BAW2881 (NVP-BAW2881) VEGFR inhibitor

Cat.No.S8189

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) VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 424.38

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (197.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 424.38 Formula

C22H15F3N4O2

 Storage (From the date of receipt)
CAS No. 861875-60-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC(=NC=C4)N)C(F)(F)F

Mechanism of Action

Targets/IC50/Ki
hVEGFR2
(Cell-free assay)
9 nM
C-Raf-1
(Cell-free assay)
24 nM
B-RAFV599E
(Cell-free assay)
76 nM
c-Abl
(Cell-free assay)
99 nM
mVEGF2
(Cell-free assay)
165 nM
RET
(Cell-free assay)
410 nM
hVEGFR3
(Cell-free assay)
420 nM
hVEGFR1
(Cell-free assay)
820 nM
In vitro
In vitro studies demonstrated that BAW2881 (NVP-BAW2881) inhibited proliferation, migration, and tube formation of human umbilical vein endothelial cells and lymphatic endothelial cells.
In vivo
BAW2881 (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 this compound 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 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.
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