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.
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 |
Molecular Weight | 424.38 |
Formula | C22H15F3N4O2 |
CAS Number | 861875-60-7 |
Solubility (25°C) | DMSO: ≥ 60 mg/mL Ethanol 20 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Related VEGFR/PDGFR Products |
---|
Isolinderalactone
Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP). |
Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
KLTWQELYQLKYKGI
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. |
Protein LMWP
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. |
CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.