VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50 for VEGFR on human hepatoma cells is 0.061 μM). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT in cells, upregulates BAX and caspase-3, and downregulates Bcl-2, thereby promoting apoptosis. VEGFR-2/AKT-IN-2 arrests the cell cycle at the S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human hepatoma cells.

Physicochemical Properties

Molecular Formula	C25H16FN5S
Molecular Weight	437.49
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 0.061 μM (IC50); Bcl-2 Caspase 3
ln Vitro	VEGFR-2/AKT-IN-2 has VEGFR2 inhibitory activity similar to that of sorafenib, with an IC50 of 0.061 μM[1]. VEGFR-2/AKT-IN-2 (0.39-100 μM, 48 h) inhibits the growth of HepG-2 and HuH-7 cell lines with IC50 values of 0.75 and 3.43 μM, respectively[1]. VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) reduces total and phosphorylated AKT in HepG-2 cells[1]. VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) promotes cell apoptosis, increases the proportion of early and late apoptotic cells (from 0.39% to 26.28% and from 0.21% to 18.87%, respectively), upregulates BAX and caspase-3, and downregulates Bcl-2[1]. VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) blocks cell cycle progression in HepG-2 cells at the S phase [1].
Cell Assay	Cell Cytotoxicity Assay[1] Cell Types: HepG-2, HuH-7, THLE-2 Tested Tested Concentrations: 100 μM, 25 μM, 6.25 μM, 1.56 μM, and 0.39 μM. Incubation Duration: 48 h Experimental Results: Inhibited the growth of HepG-2 and HuH-7 Cell Typess with IC50 of 0.75 μM and 3.43 μM, respectively. Cell Cycle Analysis[1] Cell Types: HepG-2 Tested Tested Concentrations: 0.75 μM Incubation Duration: 48 h Experimental Results: The cell cycle progression was arrested during the S phase in 48.02% of HepG-2 cells compared to untreated HepG-2 cells (29.66%). Significantly decreased the proportion of cells in the G2/M phase (58.71%) and increased the proportion of cells in the S phase after 24 h.
References	[1]. Exploring a novel thiazole derivatives hybrid with fluorinated-indenoquinoxaline as dual inhibitors targeting VEGFR2/AKT and apoptosis inducers against hepatocellular carcinoma with docking simulation. Bioorganic chemistry. 2024, 154, 108023.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2858 mL	11.4288 mL	22.8577 mL
	5 mM	0.4572 mL	2.2858 mL	4.5715 mL
	10 mM	0.2286 mL	1.1429 mL	2.2858 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.