Molecular Formula | C22H15F3N4O2 |
Molar Mass | 424.38 |
Solubility | DMSO: ≥ 33 mg/mL |
Storage Condition | -20℃ |
In vitro study | In vitro experiments showed that NVP-BAW2881 could inhibit the proliferation, migration and tubule formation of human umbilical vein endothelial cells and lymphatic endothelial cells. |
In vivo study | NVP-BAW2881 can target the tyrosine kinase region of murine, porcine and human VEGFR2. It can be administered orally or topically, but has not been tested in humans. In vivo tests in VEGF-A transgenic mice, oral or topical NVP-BAW2881 administration reduced moss-like inflammation of the ear skin. The skin lesions of the treated mice had reduced leukocyte infiltration, reduced epidermal hyperplasia, normal Epidermal Keratinocyte differentiation, and fewer vascular abnormalities. The blood vessels of the NVP-BAW2881-treated mice became smaller and less numerous. Compared with the control group, the ear swelling, skin inflammation, lymph node enlargement and skin erythema of the mice in the experimental group were improved. While both routes of administration are effective (oral and topical), systemic administration is more potent than topical administration. Topical application of NVP-BAW2881 reduced VEGF-A-induced vascular permeability in mouse and domestic pig skin. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.356 ml | 11.782 ml | 23.564 ml |
5 mM | 0.471 ml | 2.356 ml | 4.713 ml |
10 mM | 0.236 ml | 1.178 ml | 2.356 ml |
5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
biological activity | BAW2881 (NVP-BAW2881) is a novel VEGFR tyrosine kinase inhibitor. At concentrations of 1.0-4.3 nM, PDGFRβ was effectively inhibited by VEGFR1-3; At concentrations of 45-72 nM, PDGFRβ was inhibited by c-Kit and RET (c-RET). |
Target | Value |
hVEGFR2 (Cell-free assay) | 9 nM |
C-Raf-1 (Cell-free assay) | 24 nM |
B-RAFV599E (Cell-free assay) | 76 nM |
c-Abl (Cell-free assay) | 99 nM |
mVEGF2 (Cell-free assay) | 165 nM |