vegfr in 1

VEGFR inhibitor

VEGFR-3-IN-1 is a novel, potent, and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. It exhibits antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells.

VEGFR2-IN-1 is a selective and potent VEGFR2 inhibitor with antitumor activity that inhibits cell proliferation and migration and can be used in the study of breast cancer.

VEGFR-2/InhA-IN-1, a dual inhibitor based on pyrazole, targets InhA and VEGFR, exhibiting both anti-tuberculosis and anti-angiogenic properties. It demonstrates effective antibacterial activity against the Mycobacterium tuberculosis H37Rv strain (MIC = 6.25 μg/mL) and significantly suppresses VEGFR-2 activity (IC 50 = 15.27 nM).

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.

VEGFR/PDGFR-IN-1 (Compound 1) is an inhibitor of VEGFR with an IC50 of 0.4 μM. It can inhibit angiogenesis in HUVEC cells and holds promise for impeding tumor growth and metastasis.

VEGFR-2/AURKA-IN-1 (compound 5e) is a thiazolidin-4-one derivative with antitumor activity against glioma (IC50: 6.43 μM in LN229 cells). This compound exhibits affinity for AURKA and VEGFR-2, acting as a potential ligand. VEGFR-2/AURKA-IN-1 induces DNA strand breaks, showcasing cytotoxicity and anticancer potential.

PDGFRα/β/VEGFR-2-IN-1 (6f) is a multi-targeted tyrosine kinase inhibitor that specifically targets PDGFRα, PDGFRβ, and VEGFR-2 kinases at nanomolar concentrations.

VEGFR-2/STAT-3-IN-1 (Compound 9f) is a dual inhibitor targeting VEGFR-2 with an IC50 of 26.3 nM and STAT-3 with an IC50 of 5.63 nM. It suppresses the proliferation of cancer cells PANC1 and PC3, with IC50 values of 0.14 and 0.10 µM, respectively, and induces apoptosis in PC3 cells.

VEGFR-2/P-gp-IN-1 is a derivative of Licochalcone A, functioning as an orally active inhibitor of VEGFR-2 (IC50= 0.885 μM) and P-glycoprotein (P-gp). It combats tumor proliferation and overcomes chemotherapy resistance by simultaneously inhibiting VEGFR-2 kinase activity and the P-gp drug efflux pump. This compound suppresses the phosphorylation of VEGFR-2 and proteins in the downstream PI3K/AKT signaling pathway, induces apoptosis, arrests cells in the S phase, and inhibits invasive migration. Additionally, VEGFR-2/P-gp-IN-1 demonstrates potent in vivo antitumor activity in HeLa/DDP cell xenograft models and is applicable in cervical cancer research.

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.

Tubulin/VEGFR-2-IN-1 is a dual inhibitor of tubulin and VEGFR, with an IC50 of 1.52 μM, demonstrating anti-angiogenic properties. It exhibits potent cytotoxic effects against cancer cells, elevates ROS production in HepG-2 cells, induces apoptosis and causes G0/G1 phase arrest. Additionally, it inhibits the migration and colony formation abilities of HepG-2 cells. Tubulin/VEGFR-2-IN-1 is applicable in cancer research.

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

VEGFR-2/BRAF-IN-1, a dual inhibitor of VEGFR-2 and BRAF kinases, demonstrates potent inhibitory activity with IC50 values of 0.049 µM for VEGFR-2, 0.063 µM for BRAF V600E, and 0.005 µM for BRAF WT. It effectively induces apoptosis and arrests the cell cycle primarily at the G1/S phase.

hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX/XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), exhibiting Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2, and demonstrating anticancer activity [1].

VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2/M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [1].

VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC. It arrests the cell cycle at the S and G2 phases and induces apoptosis in HeLa cells, demonstrating an anti-angiogenic effect [1].

VEGFR-2/c-Met-IN-1 is a dual inhibitor of VEGFR-2 and c-Met, with IC50 values of 138 nM and 74 nM, respectively, demonstrating antitumor activity [1].

TIE-2/VEGFR-2 kinase-IN-1 is employed in the synthesis of TIE-2 and/or VEGFR-2 inhibitors for studying diseases associated with inappropriate angiogenesis [1].

VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT with IC50 values of 0.164 μM and 0.452 μM, respectively. It exhibits antitumor activity.

FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).

FLT3/VEGFR2-IN-1 (Compound 26) is a potent inhibitor of FLT3, VEGFR2, and HDAC, exhibiting IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM against FLT3, VEGFR2, and HDAC1, respectively. It effectively inhibits the phosphorylation of STAT3 and ERK1/2, as well as the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 demonstrates antitumor activity and is applicable in research on acute myeloid leukemia.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting PI3K (IC50: 2.21 μM) and VEGFR2 (IC50: 68 μM), which induces apoptosis and is utilized in cancer research [1].

PROTAC VEGFR-2 Degrader-1 (PROTAC-1), a specific degrader of PROTAC VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and exhibits low anti-proliferative effects on EA.hy926 cells (IC50 > 100 μM) [1].