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BAW2881

Cat. No. M8917
BAW2881 Structure
Synonym:

NVP-BAW2881

Size Price Availability Quantity
10mg USD 200 In stock
25mg USD 400 In stock
50mg USD 700 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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. NVP-BAW2881 inhibited proliferation, migration, and tube formation of human umbilical vein endothelial cells and lymphatic endothelial cells.

In vivo: 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. Studies in VEGF-A transgenic mice showed that oral and topical administration of NVP-BAW2881 strongly reduced psoriasis-like inflammation in ear skin. 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.

Protocol
Cell Experiment
Cell lines Human dermal lymphatic endothelial cells(LECs), human umbilical vein endothelial cells(HUVECs)
Preparation 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.
Concentrations 1 nmol/L to 1 mol/L
Incubation time 72 h
Animal Experiment
Animal models K14/VEGF-A TG mice
Formulation polyethylene glycol-200
Dosages 25 mg/kg/day
Administration oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 424.38
Formula C22H15F3N4O2
CAS Number 861875-60-7
Purity >98%
Solubility DMSO: ≥ 60 mg/mL
Ethanol 20 mg/mL
Storage at -20°C
References

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Bold G, et al. J Med Chem. 2016 Jan 14;59(1):132-46. PMID: 26629594.

Vascular endothelial growth factor inhibitors: investigational therapies for the treatment of psoriasis.
Weidemann AK, et al. Clin Cosmet Investig Dermatol. 2013 Sep 26;6:233-44. PMID: 24101875.

Inhibition of chronic and acute skin inflammation by treatment with a vascular endothelial growth factor receptor tyrosine kinase inhibitor.
Halin C, et al. Am J Pathol. 2008 Jul;173(1):265-77. PMID: 18535184.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BAW2881, NVP-BAW2881 supplier, VEGFR/PDGFR, inhibitors

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