vegfr2-in-2

VEGFR2-IN-2 has anti-inflammatory and analgesic activities.

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

FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.

VEGFR-2-IN-29 is a VEGFR2 inhibitor.

CAIX/VEGFR-2-IN-2 (compound 5e) is a dual-target inhibitor with potent inhibitory effects on CAIX (KI=3.1 μM) and VEGFR-2 (IC50=32.1 nM). This compound is applicable in research involving pancreatic cancer (PANC1), breast cancer (MCF7), and prostate cancer cells (PC3).

VEGFR-2-IN-23 (compound 11b) is a highly potent and selective inhibitor of VEGFR-2, with an IC50 value of 0.34 nM. It demonstrates significant antitumor activity by inducing apoptosis and causing cell cycle arrest at the G1 phase [1].

VEGFR-2-IN-20 (Compound 7) is a potent VEGFR inhibitor with significant potential for cancer research [1].

VEGFR-2-IN-25 (compound 5d) is a potent inhibitor of VEGFR-2 with an IC50 of 12.1 nM.

VEGFR-2-IN-27 (compound 7a) is a potent VEGFR-2 inhibitor (IC50: 14.8 nM) suitable for anticancer research.

VEGFR-2-IN-26 (compound 5h) is a potent VEGFR-2 inhibitor (IC50: 15.5 nM) that exhibits significant anti-proliferative effects on leukemia, CNS, non-small lung, ovarian, renal, prostate, and breast cancer cells.

VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor (IC50: 0.22 μM) useful for tumor research.

VEGFR-2-IN-28 is a potent inhibitor of VEGFR-2 (IC50: 0.83 μM). VEGFR-2-IN-28 induces apoptosis and exhibits antitumor effects.

VEGFR-2-IN-22 (Compound 25) is an inhibitor of VEGFR-2 and β-tubulin polymerization, with an IC50 of 19.82 nM for VEGFR-2, and is capable of inducing apoptosis.

VEGFR-2-IN-21 is a potent inhibitor of VEGFR-2 (IC50: 0.10 μM) and exhibits anticancer effects.

Compound 8g (hCA/VEGFR-2-IN-2) is an indolinonylbenzenesulfonamide identified as a potential dual inhibitor targeting cancer-associated isozymes hCA IX/XII and the angiogenic receptor VEGFR-2. It demonstrates VEGFR-2 inhibition with an IC50 of 204 nM and high affinity for hCAs, exhibiting Kis of 3.6 nM for hCA IX, 16.1 nM for hCA II, 16.7 nM for hCA XII, and 75.3 nM for hCA I. Furthermore, compound 8g exhibits antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor with an IC50 of 7 nM, suitable for breast cancer research.

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

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-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.

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-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-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.