BAW2881 (NVP-BAW2881)

Catalog No.S8189

BAW2881 (NVP-BAW2881) Chemical Structure

Molecular Weight(MW): 424.38

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 at 45-72 nM concentrations.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 at 45-72 nM concentrations.
Targets
TIE-2 [1] hVEGFR2 [1] C-Raf-1 [1] B-RAFV599E [1] c-Abl [1]
9 nM 24 nM 76 nM 99 nM
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

Cell Research:

[3]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: K14/VEGF-A TG mice
  • Formulation: polyethylene glycol-200
  • Dosages: 25 mg/kg/day
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (197.93 mM)
Ethanol 20 mg/mL (47.12 mM)
Water <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 424.38
Formula

C22H15F3N4O2

CAS No. 861875-60-7
Storage powder
in solvent
Synonyms N/A

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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.

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VEGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID