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.

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.

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET TIE-2 VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

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.

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

AMG-Tie2-1 is a potent inhibitor of endothelial endothelial cell kinase 2 (Tie2) and VEGFR2 with anticancer and antitumor activity that affects cardiovascular production, and may be used in the study of cardiovascular disease and cancer.

Brivanib Alaninate (BMS-582664) is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression.

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

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].

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).

CAY10781 is an inhibitor of the protein-protein interaction between neuropilin-1 (NRP-1) and VEGF-A.1It inhibits the interaction by 43% when used at a concentration of 12.5 μM. CAY10781 also inhibits VEGF-A-induced phosphorylation of VEGFR2 in catecholamine A-differentiated (CAD) cells when used at the same concentration. 1.Perez-Miller, S., Patek, M., Moutal, A., et al.In silico identification and validation of inhibitors of the interaction between neuropilin receptor 1 and SARS-CoV-2 Spike proteinbioRxiv308783(2020)

Su1498 (Tyrphostin SU 1498) is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), having negligible activity at several other serine threonine and tyrosine kinases.1, 2 It effectively blocks signaling through VEGFR2 both in vitro and in vivo.1, 3 SU 1498 is used to study the role of VEGFR2 signaling in diverse processes, including angiogenesis, tumor growth, neural progenitor cell survival, and neuroregeneration.

Cpd27 (TIE-2 VEGFR-2 kinase-IN-2) is a TIE-2 and VEGFR-2 inhibitor that inhibits RIPK1 and protects RGCs from TNF-stimulated cell death and can be used to study glaucoma.

ZD-4190 is a compound that inhibits both the vascular endothelial growth factor receptor 2 (VEGFR2) and the epidermal growth factor receptor (EGFR) signaling pathways, utilized in cancer treatment.