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VEGFR-2 inhibition

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

1

Peptides

1

Inhibitory Antibodies

4

Natural
Products

Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-13016
    Cabozantinib
    Maximum Cited Publications
    57 Publications Verification

    XL184; BMS-907351

    		 VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib
  • HY-112780
    UC2288
    5+ Cited Publications

    		 MDM-2/p53 Apoptosis Cancer
    UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
    UC2288
  • HY-N0876
    Arenobufagin
    4 Publications Verification

    		 Apoptosis Autophagy PI3K Akt mTOR PARP Caspase Atg8/LC3 Cancer
    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway .
    Arenobufagin
  • HY-N1408
    trans-Trimethoxyresveratrol

    trans-trismethoxy Resveratrol; (E)-Resveratrol trimethyl ether; trans-3,5,4'-Trimethoxystilbene

    		 VEGFR Reactive Oxygen Species (ROS) Caspase Apoptosis Inflammation/Immunology Cancer
    Trans-Trimethoxyresveratrol (trans-trismethoxy Resveratrol; (E)-Resveratrol trimethyl ether; trans-3,5,4'-Trimethoxystilbene) is an orally active natural derivative of Resveratrol (HY-16561). Trans-Trimethoxyresveratrol has an enhanced anticancer profile compared to Resveratrol, exhibiting higher potency than resveratrol, with improved cancer cell proliferation inhibition, induction of cell cycle arrest, decreased metastasis, and increased apoptosis. Trans-Trimethoxyresveratrol causes microtubule disassembling and tubulin depolymerization and exerts anti-angiogenic effects through VEGFR2. Trans-Trimethoxyresveratrol can be used for the studies of anti-angiogenic and anti-cancer (such as non-small cell lung cancer and osteosarcoma) .
    trans-Trimethoxyresveratrol
  • HY-13016R
    Cabozantinib (Standard)

    XL184 (Standard); BMS-907351 (Standard)

    		 Reference Standards VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib (Standard)
  • HY-146368
    PROTAC VEGFR-2 degrader-1

    		PROTACs VEGFR Cancer
    PROTAC VEGFR-2 degrader-1（PROTAC-1）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM) .
    PROTAC VEGFR-2 degrader-1
  • HY-13016A
    Cabozantinib hydrochloride

    XL184 hydrochloride; BMS-907351 hydrochloride

    		 VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib hydrochloride
  • HY-150027
    Multi-kinase-IN-3

    		VEGFR PDGFR Cancer
    Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively .
    Multi-kinase-IN-3
  • HY-178942
    EGFR/VEGFR2-IN-9

    		VEGFR EGFR Apoptosis Bcl-2 Family Caspase MDM-2/p53 Cancer
    EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers .
    EGFR/VEGFR2-IN-9
  • HY-145849
    VEGFR2-IN-1

    		VEGFR Cancer
    VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
    VEGFR2-IN-1
  • HY-W800162
    VEGFR-2-IN-37

    		VEGFR Cancer
    VEGFR-2-IN-37 (compound 12) is an inhibitor of VEGFR-2. The inhibition rate at 200 μM was approximately 56.9 μM. VEGFR-2-IN-37 is a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation .
    VEGFR-2-IN-37
  • HY-178004
    VEGFR-2-IN-73

    		VEGFR Apoptosis Cancer
    VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
    VEGFR-2-IN-73
  • HY-163125
    BHEPN

    		VEGFR Cancer
    BHEPN is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). BHEPN has inhibition of VEGFR-2 with an IC50 value of 0.320 μM. BHEPN also exhibits remarkable cytotoxic effects against HepG2 and MCF-7 cancer cell lines, with IC50 values of 0.19 μM and 1.18 μM, respectively. BHEPN can be used for anticancer research .
    BHEPN
  • HY-145864
    VEGFR-2-IN-12

    		VEGFR Cancer
    VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC50 of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI50=1.6 µM). VEGFR-2-IN-12 has antitumor activity .
    VEGFR-2-IN-12
  • HY-163533
    CPD-002

    		VEGFR Inflammation/Immunology
    CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .
    CPD-002
  • HY-175220
    4-TCPA

    		VEGFR Apoptosis EGFR mTOR Cancer
    4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia .
    4-TCPA
  • HY-164413
    CLM3

    		VEGFR EGFR RET Apoptosis Cancer
    CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
    CLM3
  • HY-152120
    (±)-Aiphanol

    Aiphanol

    		 COX VEGFR Inflammation/Immunology Cancer
    (±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak .(±)-Aiphanol effectively inhibits VEGFR2 (IC50=0.92 μM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active .
    (±)-Aiphanol
  • HY-178005
    EGFR-IN-174

    		EGFR VEGFR Apoptosis Cancer
    EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
    EGFR-IN-174
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214
  • HY-N0876R
    Arenobufagin (Standard)

    		Reference Standards Apoptosis Autophagy PI3K Akt mTOR PARP Caspase Atg8/LC3 Cancer
    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway .
    Arenobufagin (Standard)
  • HY-117039
    YM-359445 dihydroxybutanedioate

    		VEGFR Cancer
    YM-359445 dihydroxybutanedioate is an orally active VEGFR2 tyrosine kinase inhibitor, with an IC50 of 8.5 nM. YM-359445 dihydroxybutanedioate shows a complete inhibition of vascular permeability induced by VEGF. YM-359445 dihydroxybutanedioate shows antitumor activity against both lung cancer and Paclitaxel (HY-B0015)-resistant colon cancer .
    YM-359445 dihydroxybutanedioate
  • HY-P11198
    AC-P19M

    		Apoptosis VEGFR ERK Akt Caspase Bcl-2 Family Cancer
    AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research .
    AC-P19M
  • HY-141685
    3-Methylthienyl-carbonyl-JNJ-7706621

    		CDK GSK-3 VEGFR FGFR Cancer
    3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer .
    3-Methylthienyl-carbonyl-JNJ-7706621
  • HY-13590
    CEP-7055

    		VEGFR Cancer
    CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
    CEP-7055
  • HY-178968
    VEGFR-2-IN-76

    		VEGFR Cancer
    VEGFR-2-IN-76 (Compound GL-3) is a potent VEGFR-2 inhibitor with an IC50 value of 5.44 μM. VEGFR-2-IN-76 can be used for cancer research .
    VEGFR-2-IN-76
  • HY-183616
    VEGFR-2-IN-87

    		VEGFR Cancer
    VEGFR-2-IN-87 is a VEGFR-2 inhibitor with an inhibition rate of 79% in enzymatic assays. VEGFR-2-IN-87 exhibits anti-angiogenic activity. VEGFR-2-IN-87 can be used in cancer research .
    VEGFR-2-IN-87
  • HY-P992511
    CS2009

    		PD-1/PD-L1 CTLA-4 VEGFR Cancer
    CS2009 is a trispecific antibody targeting PD-1, CTLA-4 and VEGFA. CS2009 blocks the interactions of PD-1/PD-L1, CTLA-4/CD80 and VEGFA/VEGFR2, mediates checkpoint inhibition, and suppresses tumor angiogenesis. CS2009 reactivates PD-1/CTLA-4 double-positive tumor-infiltrating T lymphocytes, induces T cell activation, enhances tumor growth inhibition, promotes vascular normalization, improves T lymphocyte infiltration, and converts the immunosuppressive tumor microenvironment into an immunocompetent one. CS2009 can be used for the research of various advanced solid tumors .
    CS2009
  • HY-119618
    R1498

    		Endogenous Metabolite Cancer
    R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
    R1498
  • HY-16265A
    JI-101 hydrochloride

    		Ephrin Receptor PDGFR VEGFR Cancer
    JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
    JI-101 hydrochloride
  • HY-180827
    VEGFR-2-IN-79

    		VEGFR Apoptosis Cancer
    VEGFR-2-IN-79 (Compound 17) is a VEGFR-2 inhibitor with an IC50 of 2.32 μM. VEGFR-2-IN-79 exhibits potent and broad-spectrum cytotoxicity and can induce apoptosis in MCF-7 cells. VEGFR-2-IN-79 does not cause a significant decrease in the mitochondrial membrane potential of MCF-7 cells. VEGFR-2-IN-79 can be used for research on breast cancer .
    VEGFR-2-IN-79

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