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VEGFR

VEGF receptors are receptors for vascular endothelial growth factor (VEGF). There are three main subtypes of VEGFR, numbered 1, 2 and 3. Also, they may be membrane-bound (mbVEGFR) or soluble (sVEGFR), depending on alternative splicing.

  • Regorafenib
    T1792755037-03-7
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
    • $30
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  • AZD4547
    T19481035270-39-3
    AZD4547, a new-type specific FGFR inhibitor, targets for FGFR1 2 3 (IC50: 0.2 2.5 1.8 nM in cell-free assays).
    • $33
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  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
    • $34
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  • Tesevatinib
    TQ0166781613-23-8
    Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
    • $109
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    TargetMol | Inhibitor Hot
  • Ribociclib
    T61991211441-98-3
    Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM).
    • $36
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  • Bevacizumab
    T9904216974-75-3
    Bevacizumab, a humanized monoclonal antibody, specifically and with high affinity binds to all isoforms of VEGF-A.
    • $129
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    TargetMol | Inhibitor Hot
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  • Cabozantinib
    T2586849217-68-1
    Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.
    • $39
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    TargetMol | Inhibitor Hot
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  • Lenvatinib
    T0520417716-92-8
    Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.
    • $40
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  • Pazopanib
    T0097L444731-52-6
    Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
    • $42
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  • GSK1904529A
    T60031089283-49-7In house
    GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
    • $34
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  • Nintedanib
    T1777656247-17-5
    Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
    • $38
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  • Sanguinarine chloride
    T01295578-73-4
    Sanguinarine chloride (Pseudochelerythrine chloride), a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).
    • $50
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  • Tanshinone IIA
    T2906568-72-9
    Tanshinone IIA (Tanshinone B)(Tanshinone B) is the diterpene quinone in Danshen, which is utilized in the treatment of cardiovascular and inflammatory.
    • $50
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  • CP-547632
    T10870L252003-65-9In house
    CP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.
    • $30
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  • Taxifolin
    T1738480-18-2
    Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.
    • $46
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  • (E)-FeCP-oxindole
    T22755884338-18-5In house
    (E)-FeCP-oxindole is an inhibitor of VEGFR2 with IC50 of 214 nM.
    • $111
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  • TIE-2/VEGFR-2 kinase-IN-5
    T798601014407-83-0In house
    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.
    • $195
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  • MMPP
    T280771895957-18-2In house
    MMPP is a novel VEGFR2 inhibitor with anti-inflammatory and potential anticancer activity, inhibits STAT3, inhibits angiogenesis via VEGFR2/AKT/ERK/NF-kappaB pathway, and can be used to alleviate myocardial injury.
    • $257
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  • BGB-102
    T10531807640-87-5
    BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.
    • $328
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  • (Rac)-SAR131675
    T36911092539-44-0
    (Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol L) and VEGFR-3 autophosphorylation (IC50: 45 nmol L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.
    • $50
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  • N-Desethylsunitinib hydrochloride
    T12145L1261432-05-6
    N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.
    • $133
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  • VEGFR-2-IN-9
    T10123408502-06-7In house
    VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor (IC50: 7 nM). It can be used to study breast cancer.
    • $700
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  • VEGFR2-IN-1
    T618992765224-55-1In house
    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.
    • $293 TargetMol
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  • SU 4981
    T60094186610-88-8
    SU 4981 is an inhibitor of VEGFR and a modulator of tyrosine kinase activity.
    • $195
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  • GW297361
    T75163388627-21-2
    GW297361 is a potent inhibitor of the cell cycle protein-dependent kinase Cdk1 and also inhibits the Pho85 signaling pathway.The IC50s of GW297361 on yeast Cdk1 and Pho85 were 20 nM and 400 nM, respectively.
    • $247
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  • Cabozantinib hydrochloride
    T51641817759-42-4
    Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
    • $37
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  • (Z)-Semaxinib
    T2496194413-58-6
    (Z)-Semaxinib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. (Z)-Semaxinib is a quinolone derivative with potential antineoplastic activity.
    • $52
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  • UNC0064-12 hydrochloride (1430089-64-7(free base))
    T2056L
    UNC0064-12 hydrochloride is an inhibitor of VEGFR2.
    • $133
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  • Compound Lup-20(29)-en-3-yl acetate
    TC0036
    Lupeol acetate, a derivative of Lupeol, inhibits the progression of rheumatoid arthritis by downregulating TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
    • $89
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  • AKB-6899
    T297971007377-55-0In house
    AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.
    • $68
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  • CGP77675
    T30855234772-64-6In house
    CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.
    • $43
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  • TG 100801
    T13157867331-82-6In house
    TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).
    • $84
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  • ZM323881 hydrochloride
    T1991193000-39-4In house
    ZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.
    • $66
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  • TG 100572 Hydrochloride
    T13156L867331-64-4In house
    TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).
    • $399
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  • WAY-600
    T67301062159-35-6In house
    WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1 P-S6K(T389) and mTORC2 P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
    • $32
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  • VEGFR-3-IN-1
    T729242756668-73-0In house
    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.
    • $163
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  • (Z)-FeCP-oxindole
    T235541137967-28-2In house
    (Z)-FeCP-oxindole is a selective inhibitor of VEGFR2 with an IC50 of 200 nM for human. (Z)-FeCP-oxindole shows anticancer activity.
    • $39
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  • PKI-166
    T16549187724-61-4In house
    PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
    • $51
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  • AST 487
    T4053630124-46-8
    AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
    • $31
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  • SAR131675
    T60121433953-83-3
    SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
    • $30
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  • Sorafenib tosylate
    T0093475207-59-1
    Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
    • $37
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  • PP121
    T24151092788-83-4
    PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
    • $51
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  • (Z)-Guggulsterone
    T1728039025-23-5
    (Z)-Guggulsterone inhibits the growth of human prostate cancer cells by causing apoptosis. Z-guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis.
    • $91
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  • Axitinib
    T1452319460-85-0
    Axitinib (AG-013736) is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.
    • $33
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  • OSI-930
    T2624728033-96-3
    OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
    • $47
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  • Royal Jelly acid
    T325014113-05-4
    Royal Jelly acid (Queen Bee Acid) is an inhibitor of VEGF-induced angiogenesis, cell migration and proliferation.
    • $43
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  • Cediranib
    T2500288383-20-0
    Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.
    • $35
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  • Vandetanib
    T1656443913-73-3
    Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.
    • $45
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  • Alectinib
    T19361256580-46-7
    Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.
    • $39
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  • Ningetinib
    TQ00211394820-69-9
    Ningetinib (CT-053) (CT053PTSA) is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.
    • $42
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