vegfr2in5

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

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.

EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2, exhibiting an IC50 value of 1.15 µM for VEGFR2 and 0.28 µM for EGFRT790M. This compound demonstrates significant anticancer activity.

hCA/VEGFR-2-IN-5 (compound 9) is an indolinone phenylsulfonamide and a potential dual inhibitor of hCA IX/XII and VEGFR-2, which are associated with cancer. The compound has IC50 values of 0.38 μM for VEGFR-2, 40 nM for hCA IX, and 3.2 nM for hCA XII. It exhibits antitumor activity.

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

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.