vegfr

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.

VEGFR-3-IN-1 is a novel potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM.VEGFR-3-IN-1 possesses 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. MB-436 cells and inhibited the proliferation and migration of human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231 and MDA-MB-436 cells.

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].

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].

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 inhibitor

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

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

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-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-IN-V is a potent, vascular endothelial growth factor receptor-2 (VEGFR-2) tyrosine kinase inhibitor.

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

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

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-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-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].

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-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].

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.

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].

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].

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.

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).

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/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].

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-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-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-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].