vegfr-2-in-5

VEGFR-2-IN-5 (UNC0064-12), multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

VEGFR-2-IN-5 hydrochloride is a potent inhibitor of VEGFR2.

TIE-2 VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

VEGFR-2-IN-57 (compound 6n) exhibits significant cytotoxicity on HUVEC cells, with an IC50 value of 28.77 nM.

VEGFR-2-IN-53 (Compound 15w) is an inhibitor of VEGFR-2 with an IC50 value of 4.34 μM. It induces cell apoptosis (Apoptosis) and inhibits angiogenesis by blocking VEGFR-2 activity and preventing cell migration. Additionally, it shows an IC50 of 3.87 μM in inhibiting the growth of MCF-7 cells, making it pertinent for research in cancer therapeutics.

VEGFR-2-IN-55 (Compound 30) is an effective VEGFR-2 kinase inhibitor with an IC50 of 1.24 nM and exhibits anti-tumor activity.

VEGFR-2-IN-56 (compound 12e) exhibits the strongest inhibition activity against VEGFR-2, with an IC50 value of 45.9 nM.

VEGFR-2-IN-59 (Compound 3h) is an inhibitor of VEGFR2 with an IC50 of 3.73 µM. It exhibits cytotoxicity in cancer cell lines A549, HT-29, A375, MCF7, and NHDF, with IC50 values of 20.91, 19.70, 9.63, 17.43, and 20.71 μM, respectively. VEGFR-2-IN-59 also inhibits tubular structure formation and demonstrates anti-angiogenic properties.

VEGFR-2-IN-58 (Compound 7b) is a VEGFR-2 inhibitor with an IC50 of 42.5 nM. It shows selective cytotoxicity against cancer cells, induces cell cycle arrest at the G2 M phase, and triggers apoptosis by increasing BAX expression and decreasing Bcl2 expression. Additionally, VEGFR-2-IN-58 hampers cancer cell wound closure.

VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer with an IC50 of 0.33 μM. It exhibits growth inhibitory activity against the MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, making it a promising agent for breast cancer research.

VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) that exhibits antitumor activity. This compound induces apoptosis in tumor cells by reducing mitochondrial membrane potential and increasing levels of reactive oxygen species (ROS). Additionally, VEGFR-2-IN-51 suppresses angiogenesis through inhibition of the VEGFR-2 PI3K AKT signaling pathway. Moreover, it demonstrates significant antiproliferative effects on the gastric cancer cell line MGC-803 (IC50=0.005 μM).

VEGFR-2-IN-52 (compound 14d) serves as a powerful inhibitor of VEGFR-2, exhibiting an IC 50 of 191.1 nM. It effectively reduces the protein expression levels of p-VEGFR-2, MMP9, p-ERK1 2, and p-MEK1. In addition, VEGFR-2-IN-52 demonstrates cytotoxic properties by inducing apoptosis and arresting the cell cycle at the G0 G1 phase, and it enhances the levels of ROS.

VEGFR-2 AKT-IN-2 (Compound 5) is an inhibitor of VEGFR-2 AKT, with an IC50 of 0.061 μM for VEGFR in human liver cancer cells. It reduces total and phosphorylated AKT in cells, increases BAX and caspase-3 levels, and decreases Bcl-2, thereby inducing apoptosis. Additionally, VEGFR-2 AKT-IN-2 halts the cell cycle at the S phase and inhibits the growth of human liver cancer cells.

VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, effectively inhibiting the growth of HepG2 cells in the Pre-G1 phase and inducing apoptosis.

ODM-203 sodium is an orally available, selective, and efficient FGFR and VEGFR inhibitor, with antitumor activity, inhibiting FGFR3 1 2 and VEGFR3 2 1 4, inducing antitumor immunity, useful in solid tumor research.

VEGFR-2-IN-39 (PROTAC-5), a PROTAC that targets VEGFR-2 with an IC 50 of 208.6 nM, demonstrates low toxicity. It effectively inhibits the proliferation of EA.hy926, a type of HUVEC, in a concentration-dependent manner, achieving an IC 50 value of 38.65 µM [1].