vegfr-2-in-6

VEGFR-2-IN-6 (WO 02/059110, example 64) is a potent inhibitor of VEGFR2, a crucial receptor involved in the regulation of angiogenesis [1].

VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 of 0.509 µM and an IC50 value of 7.48 μM for inhibiting MCF-7 cell proliferation. Its anticancer activity is exerted through cell cycle arrest, induction of apoptosis (Apoptosis), and modulation of gene expression, making it suitable for breast cancer research.

VEGFR-2-IN-69 (Compound 5A) is an inhibitor of VEGFR-2 and telomerase (Telomerase) that enhances the expression of caspase 3, caspase 8, and caspase 9, while reducing the levels of CDK-2, CDK-4, and CDK-6. It has an IC50 of 15.46 µM against HCT116.

VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.

VEGFR-2-IN-60 (compound 5c) is a potent VEGFR-2 inhibitor with an IC50 of 1.07 nM and exhibits cytotoxic activity against HCC1806, Hela, and A549 cell lines.

VEGFR-2-IN-62 (Compound 3f) is a potent inhibitor of VEGFR-2, with an IC50 value of 0.0557 μM. It inhibits cell proliferation and induces apoptosis (Apoptosis), making it useful for cancer research.

VEGFR-2-IN-63 (Compound 12b) is an inhibitor of VEGFR2, reducing 87.2% of VEGFR-2 activity at 10 μM. It exhibits anti-proliferative activity against various cancer cells, with IC50 values of 6.5 μM for HCT116, 2.1 μM for MCF7, and 4.1 μM for PaCa2.

VEGFR-2-IN-61 (Compound 7b) is an inhibitor of VEGFR-2 with an IC50 of 2.83 µM. It effectively inhibits the proliferation of various cancer cells, including MCF-7 cells, with an IC50 of 2.12 µM. Additionally, VEGFR-2-IN-61 suppresses cell migration and induces oxidative stress and apoptosis in MCF-7 cells.

VEGFR-2-IN-65 (Compound 07) functions as a VEGFR-2 inhibitor. It forms hydrogen bonds with Cys180 and can inhibit tube formation in HUVECs.

VEGFR-2-IN-67 (Compound 6b) functions as an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), with IC50 values of 5.91 µM for MDA-231 cells and 7.16 µM for MCF-7 cells. Its inhibitory activity on VEGFR-2 is comparable to Sorafenib (IC50 of 53.63 nM). VEGFR-2-IN-67 exhibits significant anticancer activity by inducing cell apoptosis (with an early apoptosis rate of 57.20%), causing G1 phase cell cycle arrest, upregulating pro-apoptotic markers, and downregulating Bcl-2. This compound is utilized in cancer research.

VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.

EGFR/VEGFR2-IN-6 (Compound 3k) is a dual inhibitor targeting EGFR and VEGFR2, exhibiting IC50 values of 10.53 μM for EGFR and 3.37 μM for VEGFR2. It demonstrates significant antiproliferative activity against breast cancer cells and induces G0/G1 cell cycle arrest and apoptosis, particularly early apoptosis. EGFR/VEGFR2-IN-6 is applicable in cancer research.

VEGFR-2-IN-40 is a VEGFR-2 inhibitor. It stimulates both early and late apoptosis. Additionally, VEGFR-2-IN-40 reduces the levels of immunomodulatory proteins TNF-α and IL-6, while increasing the apoptosis marker caspase-3 fourfold.

EGFRT790M/VEGFR-2-IN-1 (Compound 6) is a dual inhibitor targeting the EGFRT790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM). It effectively blocks tumor cell proliferation and angiogenesis signaling pathways. This compound exhibits potent cytotoxicity against various cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM) and holds potential for research in non-small cell lung cancer and solid tumors.

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.