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Angiogenesis

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Items 1-50 of 1495

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  1. A10108
    Saracatinib (AZD0530)

    Src/Abl inhibitor

    Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.
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  2. A15801
    Entrectinib

    TRK, ROS1, ALK inhibitor

    Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.
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  3. A12694
    Pacritinib (SB1518)

    JAK2/FLT3 inhibitor

    Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.
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  4. A10001
    Sorafenib Tosylate (Nexavar)

    Raf inhibitor

    Sorafenib Tosylate (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
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  5. A10699
    Pazopanib HCl (GW786034)

    VEGFR/PDGFR/FGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
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  6. A11496
    Motesanib (AMG706)

    VEGFR Inhibitor

    Motesanib (AMG706) is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors with IC?? values of 2 nM (VEGFR1), 3 nM (VEGFR2), 6 nM (VEGFR3), 84 nM (PDGFR), and 8 nM (Kit).
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  7. A10967
    Vatalanib (PTK787) 2HCl

    VEGFR inhibitor

    Vatalanib (PTK787 or PTK/ZK) is a small molecule protein kinase inhibitor that inhibits angiogenesis that inhibits all known VEGF receptors, as well as platelet-derived growth factor receptor-beta and c-kit, but is most selective for VEGFR-2. CAS: 212141-51-0 (HCl) 212141-54-3 (Free base)
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  8. A10953
    TSU-68 (Orantinib, SU6668)

    PDFGRβ inhibitor

    Orantinib (TSU-68, SU6668) has greatest potency against PDGFR autophosphorylation with Ki of 8 nM in a cell-free assay, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. Phase 3.
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  9. A10963
    Vandetanib (ZD6474)

    VEGFR inhibitor

    Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
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  10. A10254
    Brivanib (BMS-540215)

    VEGFR-2 inhibitor

    Brivanib (BMS-540215) is a VEGFR -2 inhibitor with an IC50 of 25 nM and Ki of 26 nM.
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  11. A10025
    Linifanib (ABT-869)

    VEGFR/PDGFR inhibitor

    Linifanib (ABT-869) is a structurally novel, potent inhibitor of RTK, VEGF and PDGF with IC50 of 0.2, 2, 4, and 7 nM for human endothelial cells, PDGFR-β, KDR, and CSF-1R, respectively.

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  12. A10185
    Cediranib (AZD2171)

    VEGFR inhibitor

    Cediranib (AZD2171) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.
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  13. A10101
    Tivozanib (AV-951)

    VEGFR Inhibitor

    Tivozanib (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor that is designed to inhibit all three VEGF receptors.
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  14. A10998
    Foretinib (GSK1363089, XL880)

    c-MET inhibitor

    Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.
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  15. A10043
    AEE788

    EGFR inhibitor

    AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.
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  16. A14213
    EW-7197 (Vactosertib)

    ALK4/ALK5 inhibitor

    EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively
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  17. A16245
    Crizotinib hydrochloride

    c-Met/NPM-ALK inhibitor

    Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.
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  18. A10703
    PD173074

    FGFR1/VEGFR2 Inhibitor

    PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR.
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  19. A15271
    Vandetanib HCl

    VEGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
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  20. A11235
    PF 573228

    FAK Inhibitor

    PF 573228 is a potent and selective inhibitor of focal adhesion kinase (FAK) (IC50 = 4 nM).
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  21. A12580
    PF-00562271

    FAK inhibitor

    PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.
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  22. A11020
    PCI-32765 (Ibrutinib)

    Bruton tyrosine kinase inhibitor

    PCI-32765 is an orally bioavailable small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
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  23. A10211
    Canertinib (CI-1033)

    HER2/ErbB2 inhibitor

    Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).
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  24. A11158
    ARRY334543 (Varlitinib)

    EGFR inhibitor

    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
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  25. A11416
    Erlotinib

    EGFR inhibitor

    Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
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  26. A10422
    Gefitinib (Iressa)

    EGFR Inhibitor

    Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
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  27. A13998
    DMOG

    HIF-PH inhibitor

    DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.
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  28. A15186
    Nilotinib monohydrochloride monohydrate

    Bcr-Abl inhibitor

    Nilotinib is a Bcr-Abl inhibitor with IC50 less than 30 nM.
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  29. A11200
    DCC-2036 (Rebastinib)

    Bcr-Abl inhibitor

    DCC-2036 is an orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity.

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  30. A10290
    Dasatinib (BMS-354825)

    Abl-Src inhibitor

    Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2.
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  31. A18014
    Afatinib

    EGFR inhibitor

    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
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  32. A10468
    Imatinib Mesylate

    Bcr-Abl inhibitor

    Imatinib mesylate, a selective tyrosine kinase inhibitor, induced a sustained objective response in treating gastrointestinal stromal tumors with the inhibition of the KIT signal-transduction pathway.
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  33. A11192
    PF-562271

    FAK inhibitor

    PF-562271 is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities.
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  34. A15152
    Masitinib mesylate

    KIT/PDGFR inhibitor

    Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
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  35. A11350
    CP-673451

    PDGFRα/β inhibitor

    CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
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  36. A10893
    Taxifolin

    VEGFR-2 Inhibitor

    Taxifolin is found to bind at the ATP-binding site on VEGFR-2 kinase with large value of binding energy and act as type I competitive inhibitor.
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  37. A10988
    WP1130 (Degrasyn)

    DUB/Bcr/ABL Inhibitor

    WP1130 (Degrasyn) is a novel selective small molecular deubiquitinase inhibitor and a Bcr/Abl destruction pathway activator that specifically and rapidly down-regulates both wild-type and mutant Bcr/Abl protein without affecting bcr/abl gene expression in chronic myelogenous leukemia (CML) cells.
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  38. A11022
    AG-1478 (Tyrphostin AG-1478)

    EGFR Inhibitor

    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
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  39. A10502
    Ki8751

    VEGFR-2 inhibitor

    Ki8751 is a cell-permeable quinolyloxyphenyl-urea compound that acts as a Flk-1 (VEGFR-2)-selective inhibitior in both cell-based and cell-free assays.
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  40. A11518
    Pazopanib (GW-786034)

    VEGFR inhibitor

    Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
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  41. A11028
    AV-412

    EGFR inhibitor

    AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis.
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  42. A11205
    LDN193189

    ALK inhibitor

    LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.
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  43. A11952
    P505-15 (PRT062607, BIIB057)

    Syk inhibitor

    P505-15 (also known as PRT062607) is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases.
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  44. A15848
    FIIN-3

    Irreversible FGFR inhibitor

    FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.
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  45. A10250
    Regorafenib (BAY 73-4506)

    VEGFR inhibitor

    Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
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  46. A20550
    Futibatinib

    FGFR inhibitor

    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor.
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  47. A10638
    Neratinib (HKI-272)

    HER2 inhibitor

    Neratinib (HKI-272) is a tyrosine kinase inhibitor.
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  48. A10996
    XL184 free base (Cabozantinib)

    VEGFR inhibitor

    XL184 free base (Cabozantinib) is a small molecule designed to inhibit multiple receptor tyrosine kinases, specifically MET and VEGFR2.
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  49. A10340
    E7080 (Lenvatinib)

    VEGFR Inhibitor

    E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.
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  50. A17858
    Sunitinib

    multi-targeted receptor tyrosine kinase inhibitor

    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
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