VEGFR-2-IN-43
VEGFR-2-IN-43 (compound 16) is an orally active inhibitor of VEGFR2, with an IC50 of 39.91 μM. VEGFR-2-IN-43 can be used for wet age-related macular degeneration (w-AMD) disease research.
For research use only. We do not sell to patients.
- Formula: C24H27FN4O5
- Molecular Weight:470.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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VEGFR2 39.91 μM (IC50) |
VEGFR-2-IN-43 (compound 16) (0-50 μM, 72 h) demonstrates a weak inhibitory effect on proliferation of LX-2 cells, and significantly inhibits the proliferation of BaF3-Tel-VEGFR2 cells[1].
VEGFR-2-IN-43 (0-10 μM, 48 h) exhibits a concentrationdependent inhibition of VEGFR2 phosphorylation in HUVECs [1].
VEGFR-2-IN-43 (1 μM, 0-120 min) shows remarkable plasma stability and moderate liver microsomal stability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3-Tel-VEGFR2 cells, BaF3 cells (BaF3-Tel-VEGFR2 cells were constructed through viral transgene technology using BaF3 cells as a template, and their proliferation was dependent on VEGFR2 kinase.)
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Concentration:0-50 μM
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Incubation Time:72 h
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Result:The GI50 value of VEGFR-2-IN-43 (compound 16) for BAF3-tel-VEGFR2 cells was 22.9 nM, and the proliferation of BaF3 cells was almost not inhibited.
Pharmacokinetic study of VEGFR-2-IN-43 (compound 16) on mice[1]
| Route | Dose (mg/kg) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | MRT0-t (h) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | F (%) |
| i.v. | 2 | 508 | 512 | 0.665 | 853 | 0.0833 | 1.32 | / |
| p.o. | 10 | 506 | 518 | 0.72 | 321 | 0.417 | 1.58 | 20.2 |