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  • Protein Tyrosine Kinases

Protein Tyrosine Kinases

Items 1-50 of 600

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  1. 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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  2. A10005
    (-)-Epigallocatechin gallate

    Antioxidant, antiangiogenic, antitumor agent

    (-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.
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  3. 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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  4. A10027
    AC220 (Quizartinib)

    FLT3 inhibitor

    AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56±0.3 nM and >10 mM for MC4-11 and A375, respectively.

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  5. 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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  6. A10047
    AG-490

    EGFR inhibitor

    AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
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  7. A10053
    Tyrphostin AG 879

    HER2 inhibitor

    Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA.
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  8. A10062
    Allitinib tosylate (AST-1306 TsOH, AST-6)

    EGFR inhibitor

    AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo
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  9. A10063
    AMG 208

    c-Met Inhibitor

    AMG 208 is a novel c-Met inhibitor that inhibits the ligand-dependent and ligand-independent activation of c-Met, inhibiting its tyrosine kinase activity.
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  10. A10080
    AP24534 (Ponatinib)

    BCR-ABL inhibitor

    AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.
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  11. 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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  12. A10103
    Axitinib

    VEGFR inhibitor

    Axitinib is a small molecule tyrosine kinase inhibitor,which inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117).
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  13. 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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  14. A10116
    AZD8931 (Sapitinib)

    pan-EGFR/pan-erbB inhibitor

    AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.
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  15. A10137
    Bibf1120 (Nintedanib)

    VEGFR inhibitor

    BIBF1120 (Vargatef) is a novel triple angiokinase inhibitor that inhibits three growth factor receptors simultaneously: VEGFR, PDGF and FGFR.
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  16. A10141
    (E/Z)-BIBW2992 (E/Z-Afatinib)

    EGFR inhibitor

    BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.
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  17. A10153
    BMS-777607

    c-Met inhibitor

    BMS-777607 is a MET tyrosine kinase inhibitor that binds to c-Met protein, or HGFR, preventing binding of HGF and disrupting the MET signaling pathway.
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  18. A10154
    BMS-794833

    c-Met inhibitor

    BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol.
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  19. A10161
    Bosutinib (SKI-606)

    Src inhibitor

    Bosutinib (SKI-606) is a tyrosine kinase inhibitor undergoing research for use in the treatment of cancer.
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  20. A10162
    Brivanib alaninate (BMS-582664)

    VEGFR inhibitor

    Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling.
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  21. A10185
    Cediranib (AZD2171)

    VEGFR inhibitor

    Cediranib (AZD2171) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.
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  22. A10198
    Dovitinib Dilactic acid (TKI258 Dilactic acid)

    RTK inhibitor

    Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.
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  23. A10210
    Chrysophanic acid (Chrysophanol)

    EGFR inhibitor

    Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway.
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  24. 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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  25. A10242
    CP-724714

    HER2/ErbB2 inhibitor

    CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) .
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  26. A10248
    CYC116

    Aurora Kinase inhibitor

    Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis.
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  27. 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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  28. 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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  29. A10259
    Imatinib (Gleevec)

    PDGFR inhibitor

    Imatinib (Gleevec) is a number of tyrosine kinase enzymes specific inhibitor.
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  30. A10286
    Daphnetin

    EGFR, PKA,PKC inhibitor

    Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
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  31. 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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  32. A10340
    E7080 (Lenvatinib)

    VEGFR Inhibitor

    E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.
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  33. A10352
    ENMD-2076

    Aurora A / FLT3 Inhibitor

    ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
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  34. A10362
    Erlotinib HCl

    EGFR inhibitor

    Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
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  35. 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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  36. A10425
    Genistein

    EGFR inhibitor

    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
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  37. A10426
    Genistin (Genistoside)

    Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo.
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  38. A10440
    GSK1904529A

    IGF-1R inhibitor

    GSK1904529A selectively inhibits IGF-IR and IR with IC(50)s of 27 and 25 nmol/L, respectively.
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  39. 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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  40. A10493
    JNJ-38877605

    c-Met inhibitor

    c-Met inhibitor JNJ-38877605 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways.
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  41. 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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  42. A10504
    KRN 633

    VEGFR Inhibitor

    KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor that inhibits PDGFR-α and c-Kit at higher concentrations only (IC50 = 0.97 μM and 4.33 μM, respectively) and inactive towards 17 other kinases (IC50 ??? 10 μM).
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  43. A10508
    KW-2449

    FLT3/FGFR/Bcr-Abl/Aurora Inhibitor

    KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
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  44. A10514
    Lapatinib Ditosylate

    HER2 inhibitor

    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
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  45. A10558
    Masitinib ( AB1010)

    c-Kit inhibitor

    Masitinib (AB1010) is a protein tyrosine kinase inhibitor.
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  46. A10587
    MGCD-265 (Glesatinib)

    c-Met inhibitor

    MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R.
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  47. A10608
    Motesanib Diphosphate (AMG-706)

    VEGFR inhibitor

    Motesanib, also known as AMG-706, is an orally administered multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors, and Kit receptors.
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  48. A10610
    MP470 (MP-470, Amuvatinib)

    RTK inhibitor

    MP470 is a c-Kit/PDGFR tyrosine kinase inhibitor.
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  49. A10612
    Mubritinib (TAK 165)

    HER2/ErbB2 inhibitor

    Mubritinib (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5.
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  50. A10638
    Neratinib (HKI-272)

    HER2 inhibitor

    Neratinib (HKI-272) is a tyrosine kinase inhibitor.
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