VEGFR-2/AKT-IN-2 

VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC₅₀: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells^[1].

VEGFR-2/AKT-IN-2 has similar VEGFR2 (on the HepG-2 cell) inhibitory activity with an IC₅₀ value of 0.061 μM compared to Sorafenib (HY-10201) ^[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 of 0.75 and 3.43 μM, respectively, whereas the IC₅₀ for THLE-2 is 25.53 μM^[1].
VEGFR-2/AKT-IN-2 (0.75 μM) reduces both total VEGFR2 and p-VEGFR2 in treated HepG-2 cells by 38.32 % and 77.64 %, respectively^[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) reduces total and phosphorylated AKT in HepG-2 cells, respectively^[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) promotes apoptosis with increasing the percentage of early and late apoptotic cells (from 0.39% to 26.28% and from 0.21% to 18.87%, respectively), up-regulating BAX and caspase-3, and down-regulating Bcl-2^[1].
VEGFR-2/AKT-IN-2 (0.75 μM, 48 h) prevents the progression of HepG-2 cell cycle during S phase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

437.49

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• [1]. Abusaif, et al. 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.