BAW2881 (NVP-BAW2881)

Catalog No.S8189

For research use only.

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

CAS No. 861875-60-7

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

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Other VEGFR Products

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 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 Research:

[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 Research:

[3]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 424.38
Formula

C22H15F3N4O2

CAS No. 861875-60-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC(=NC=C4)N)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) supplier | purchase BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) cost | BAW2881 (NVP-BAW2881) manufacturer | order BAW2881 (NVP-BAW2881) | BAW2881 (NVP-BAW2881) distributor