TIE-2/VEGFR-2 kinase-IN-5 is a potent TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor with anti-angiogenic activity and is commonly used in biomedical research related to angiogenesis.

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor (IC50: 7 nM). It can be used to study breast cancer.

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

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

VEGFR-2-IN-37 (compound 12), a VEGFR-2 inhibitor, exhibits an inhibition rate of approximately 56.9 μM at a concentration of 200 μM. It is also identified as a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation [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].

TIE-2/VEGFR-2 kinase-IN-4, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting inhibitory concentration (IC50) values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2-IN-18 (Compound 15d) is a high-potency inhibitor of VEGFR-2, with an IC 50 value of 60 nM. This compound effectively initiates cell apoptosis and demonstrates significant antitumor properties [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.

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

VEGFR-2-IN-27 (compound 7a) is a potent inhibitor of VEGFR-2 (IC50: 14.8 nM) and can be used in anticancer studies.

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor targeting VEGFR-2 and DHFR, exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. It demonstrates effective antibacterial properties against a range of pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, this compound shows potent cytotoxic effects against various cancer cell lines such as C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, rendering it a valuable tool for cancer research [1].

VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis. Its mechanism of action involves the induction of cellular apoptosis and elevation of intracellular reactive oxygen species. Due to these properties, VEGFR-2-IN-19 holds promise as an effective anticancer agent [1].

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

VEGFR-2-IN-35 (compound 7) is a potent inhibitor of VEGFR-2, exhibiting an IC50 of 37 nM. Additionally, it demonstrates inhibitory activity against MCF-7 and HCT 116 cancer cell lines with IC50 values of 10.56 μM and 7.07 μM, respectively [1].

hCA/VEGFR-2-IN-4 (compound 15b), an indolinylbenzenesulfonamide, serves as a potential dual inhibitor targeting cancer-related human carbonic anhydrases hCA IX/XII and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits an IC50 value of 0.811 µM against VEGFR-2 and demonstrates high affinity for hCAs, with inhibition constants (Ki) of 3.8 nM for hCA XII, 6.2 nM for hCA IX, 19.8 nM for hCA II, and 35.5 nM for hCA I. Additionally, the compound shows antiproliferative effects on breast cancer cells overexpressing VEGFR-2 [1].

VEGFR-2-IN-33 (Compound 4d), a potent VEGFR inhibitor with an IC50 value of 61.04 nM, demonstrates significant inhibition of HepG2 cell proliferation, achieving an IC50 of 4.31 nM. This compound is utilized for hepatocellular carcinoma (HCC) research [1].

VEGFR-2-IN-17 (Compound 15a) is a highly potent inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2), with an IC50 value of 67.25 nM. This compound exhibits significant antitumor properties [1].

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

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

TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors that can be used for the study of diseases associated with inappropriate angiogenesis [1].

VEGFR-2-IN-16 (Compound 15b) is a potent inhibitor of VEGFR-2 (IC50: 86.36 nM) that exhibits antitumour effects.

VEGFR-2-IN-30, a compound acting primarily as a VEGFR-2 inhibitor (IC50: 66 nM), demonstrates additional inhibitory effects on PDGFR, EGFR, and FGFR1, with IC50 values of 180, 98, and 82 nM, respectively. It effectively arrests cancer cells in the S-phase and induces both early and late apoptosis.

VEGFR-2-IN-10 has enhanced antiangiogenic potency against VEGFR2 phosphorylation induced by VEGF with an IC50 value of 0.7 μM and no cytotoxic effects.

VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent inhibitor of VEGFR-2 (IC50: 0.037 μM). VEGFR-2-IN-12 has anti-tumour effects.

VEGFR-2-IN-5 hydrochloride is an effective VEGFR2 inhibitor.

VEGFR-2-IN-24 is a potent inhibitor of VEGFR-2 (IC50: 0.22 μM) and can be used to study tumors.

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

VEGFR-2-IN-36 (compound 15) serves as a potent VEGFR-2 inhibitor, exhibiting an IC50 value of 0.067 μM, and acts as an apoptosis inducer with demonstrated anticancer efficacy. It modulates apoptotic pathways by upregulating BAX and downregulating Bcl-2, leading to cytotoxic effects on cancer cell lines, including MCF-7 (IC50 = 0.42 μM) and HepG2 (IC50 = 0.22 μM) [1].

VEGFR-2-IN-32 (Comp 3a) is an inhibitor of VEGFR-2, exhibiting an inhibitory concentration (IC 50) of 8.93 nM, and demonstrates cytotoxic activity towards PC-3 cells with an IC 50 of 1.22 μM, indicating its potential utility in anti-prostate cancer research [1].

TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide with potential as a dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. This compound inhibits VEGFR-2 with an IC50 of 358 nM and exhibits high affinity for hCAs, evidenced by Ki values of 4.2 nM for hCA IX, 22.9 nM for hCA II, 25.1 nM for hCA I, and 28.0 nM for hCA XII. Additionally, hCA/VEGFR-2-IN-3 demonstrates antiproliferative activity specifically against breast cancer cells that overexpress VEGFR-2 [1].

VEGFR-2/BRAF-IN-2, as a dual VEGFR-2 and BRAF kinase inhibitor, exhibits potent IC50 values of 0.111 µM, 0.089 µM, and 0.071 µM against VEGFR-2, BRAF V600E, and BRAF WT, respectively. This compound effectively induces apoptosis and predominantly arrests the cell cycle in the G1 phase.

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).

PROTAC VEGFR-2 degrader-2 (PROTAC-4), a specific degrader of VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and low anti-proliferative activity towards EA.hy926 cells (IC50 > 100 μM) [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].

VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

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

TIE-2/VEGFR-2 kinase-IN-2 is a powerful inhibitor of both VEGFR2 and Tie-2 kinases, displaying noteworthy pIC 50 values of 8.61 and 8.56, respectively. This compound acts as an anti-angiogenic agent, making it highly relevant for cancer research.

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].

VEGFR-2-IN-31 (compound 3i), a robust VEGFR-2 inhibitor (IC50=8.93 nM), serves as an anti-prostate cancer agent by arresting the cell cycle at the S-phase and inducing apoptosis.

VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor (IC50: 3.4 nM). vEGFR-2-IN-13 arrests the HepG2 cell cycle in G2/M phase and induces apoptosis.

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-11 is a potent inhibitor of VEGFR-2 (IC50: 60.27 nM) with an IC50 value of 60.27 nM, which induces apoptosis and has anticancer activity.

VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

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

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].

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). It exhibits 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. This compound demonstrates anticancer activity [1].

Fruquintinib (HMPL-013) is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.