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| 5mg |
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| 25mg |
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Purity: ≥98%
NVP-BAW2881 (also known as BAW2881) is a novel, potent and selective VEGFR2 inhibitor with an IC50 of 4 nM. In vitro, NVP-BAW2881 caused human umbilical vein endothelial cells and lymphatic endothelial cells to proliferate, migrate, and form tubes less frequently. NVP-BAW2881 normalized the epidermal architecture and decreased the number of blood and lymphatic vessels as well as infiltrating leukocytes in the skin in a transgenic mouse model of psoriasis. In models of acute inflammation, NVP-BAW2881 also demonstrated potent anti-inflammatory properties; topical NVP-BAW2881 pretreatment markedly reduced VEGF-A-induced vascular permeability in pig and mouse skin. Moreover, topical administration of NVP-BAW2881 decreased the inflammatory reaction that contact hypersensitivity reactions or UV-B irradiation caused in pig skin. For the first time, these findings show that VEGF receptor tyrosine-kinase inhibitors may be used to treat psoriasis and other inflammatory skin conditions in patients.
| Targets |
VEGFR1 (IC50 = 820 nM); VEGFR2 (IC50 = 9 nM); VEGFR3 (IC50 = 420 nM); Tie2 (IC50 = 650 nM)
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| ln Vitro |
NVP-BAW2881 was shown to inhibit the migration, proliferation, and tube formation of lymphatic and human umbilical vein endothelial cells in in vitro studies[2].
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| ln Vivo |
NVP-BAW2881 specifically targets the human, pig, and murine VEGFR2 tyrosine kinase domain. It has not been tested on humans, but it can be applied topically or taken orally. NVP-BAW2881 was shown to significantly reduce psoriasis-like inflammation in the skin of the ears through oral and topical administration in in vivo studies conducted on VEGF-A transgenic mice. From a histological perspective, the skin lesions in the treated mice displayed fewer vascular abnormalities, decreased epidermal hyperproliferation, normalized epidermal keratinocyte differentiation, and decreased leukocyte infiltration. In treated mice, there were fewer and smaller vessels. The ear swelling, skin inflammation, lymph node enlargement, and skin erythema of treated mice were significantly improved when compared to control mice. Systemic administration of NVP-BAW2881 was more effective than topical administration, despite the effectiveness of both modes of administration. Moreover, topical NVP-BAW2881 successfully decreased VEGF-A-induced vascular permeability in mice's and domestic pigs' skin[2].
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| Cell Assay |
The fibronectin-coated 96-well plates were seeded with HUVECs or LECs (1.2×103). Subsequently, the cells were cultured for a further twenty-four hours in LEC medium supplemented with 2% fetal bovine serum. Eight wells/condition of cells were cultured in medium alone (control), with 20 ng/ml VEGF-A, or in combination with 1 nmol/L to 1 mol/L NVP-BAW2881. LECs cultured with 500 ng/ml VEGF-C underwent proliferation assay as well. In all well, the concentration of dimethyl sulfoxide was changed to 0.1%. Using a SpectraMax Gemini electron microscope, cells were incubated with 5-methylumbelliferylheptanoate for 72 hours, after which the number of viable cells was fluoresced.
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| Animal Protocol |
Mice: Eight-week-old female K14/VEGF-A TG mice have their ear skin induced to undergo a contact hypersensitivity response. Topical application of 10 μL oxazolone (1%) on each side challenges the right ear five days after sensitization (day 0). Once daily oral doses of 25 mg/kg NVP-BAW2881 or twice daily topical doses of 0.5% NVP-BAW2881 are given for 14 days, commencing on day 7. Cars are provided alone to control groups. Every other day, the thickness of the ears is measured with calipers. After 21 days, the mice are killed, and the weight of each ear and the lymph node (LN) that drains it is measured[2].
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| References |
| Molecular Formula |
C22H15F3N4O2
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|---|---|
| Molecular Weight |
424.3753
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| Exact Mass |
424.11
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| Elemental Analysis |
C, 62.26; H, 3.56; F, 13.43; N, 13.20; O, 7.54
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| CAS # |
861875-60-7
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| Related CAS # |
861875-60-7
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC(=NC=C4)N)C(F)(F)F
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| InChi Key |
MLLQJNIKDWEEFT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H15F3N4O2/c23-22(24,25)14-4-2-5-15(12-14)28-20(30)18-6-1-3-13-11-16(7-8-17(13)18)31-19-9-10-27-21(26)29-19/h1-12H,(H,28,30)(H2,26,27,29)
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| Chemical Name |
6-(2-aminopyrimidin-4-yl)oxy-N-[3-(trifluoromethyl)phenyl]naphthalene-1-carboxamide
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| Synonyms |
BAW2881; BAW 2881; BAW-2881; NVP-BAW-2881; NVP-BAW 2881; NVP-BAW2881
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~84 mg/mL (~197.9 mM)
Water: <1 mg/mL Ethanol: ~20 mg/mL (~47.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3564 mL | 11.7819 mL | 23.5638 mL | |
| 5 mM | 0.4713 mL | 2.3564 mL | 4.7128 mL | |
| 10 mM | 0.2356 mL | 1.1782 mL | 2.3564 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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