rvegfr2

Pamufetinib mesylate (TAS-115 mesylate) is a potent vascular endothelial growth factor receptor (VEGFR) antagonist and hepatocyte growth factor receptor (c-Met) inhibitor used in the study of cancer and respiratory diseases.

EGFR/VEGFR2-IN-1 (Compound 10e) serves as an inhibitor for VEGFR-2 and EGFR, with respective IC50 values of 0.26 and 0.14 μM. It inhibits microtubule protein polymerization with an IC50 of 40.9 μM and induces cell apoptosis (Apoptosis). EGFR/VEGFR2-IN-1 is applicable in research related to anti-leukemia and anti-lymphoma treatments.

EGFR/VEGFR2-IN-2 (compound 4b) serves as a dual inhibitor of VEGFR-2 and EGFR.

EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.

EGFR/VEGFR2-IN-4 (Compound 19) is an irreversible inhibitor of both EGFR and VEGFR-2, exhibiting IC50 values of 18.7 nM and 102.3 nM, respectively, under conditions of 1 μM ATP.

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.

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.

EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). It significantly suppresses the proliferation of various cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 increases the expression levels of Bax, caspase-3, and p53, while decreasing Bcl-2 expression. This compound induces apoptosis and causes cell cycle arrest at the G1 phase. It is suitable for research on anti-tumor angiogenesis and multidrug-resistant cancers.

EGFR/VEGFR2-IN-10 is a selective inhibitor of EGFR, VEGFR2, and COX2 with IC50 values of 8.5, 68, and 158 nM, respectively. This compound can induce G1 phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8 expression, and elevates caspase-9 protein levels, thereby activating the intrinsic apoptotic pathway. It demonstrates favorable selectivity by inhibiting tumor proliferation, angiogenesis, and inflammation pathways. EGFR/VEGFR2-IN-10 serves as a tool for the study of cervical cancer, liver cancer, colon cancer, and breast cancer.

Pamufetinib (TAS-115) is a potent kinase inhibitor targeting VEGFR and the hepatocyte growth factor receptor (c-Met/HGFR), with IC50s of 30 nM for rVEGFR2 and 32 nM for rMET, respectively.