VEGFR-2-IN-43 (compound 16) is an orally active VEGFR2 inhibitor with IC50 of 39.91 μM. VEGFR-2-IN-43 can be used in the study of wet age-related macular degeneration (w-AMD).

Physicochemical Properties

Molecular Formula	C24H27FN4O5
Molecular Weight	470.49
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)

Biological Activity

Targets	VEGFR2 39.91 μM (IC50)
ln Vitro	VEGFR-2-IN-43 (compound 16) (0-50 μM, 72 h) has a weak inhibitory effect on the proliferation of LX-2 cells and a significant inhibitory effect on the proliferation of BaF3-Tel-VEGFR2 cells[1]. VEGFR-2-IN-43 (0-10 μM, 48 h) exhibits concentration-dependent inhibition of VEGFR2 phosphorylation in HUVEC cells [1]. VEGFR-2-IN-43 (1 μM, 0-120 min) exhibits significant plasma stability and moderate liver microsomal stability[1].
ln Vivo	VEGFR-2-IN-43 (compound 16) (2/10 mg/kg, iv and po) showed acceptable oral bioavailability in ICR mice (F = 20.2%)[1].
Cell Assay	Cell Proliferation Assay[1] Cell Types: 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.) Tested Tested Concentrations: 0-50 μM Incubation Duration: 72 h Experimental Results: 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.
References	[1]. Potential oral VEGFR2 inhibitors: Treatment of wet age-related macular degeneration. Bioorg Chem. 2024 Mar;144:107110.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1254 mL	10.6272 mL	21.2544 mL
	5 mM	0.4251 mL	2.1254 mL	4.2509 mL
	10 mM	0.2125 mL	1.0627 mL	2.1254 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.