Protein Tyrosine Kinases

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  1. 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
  2. c-Met inhibitor

    BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol.
  3. 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.
  4. RTK inhibitor

    MP470 is a c-Kit/PDGFR tyrosine kinase inhibitor.
  5. IGF-1R inhibitor

    NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM.
  6. EGFR Inhibitor

    OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .
  7. Aurora inhibitor

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
  8. Syk Inhibitor

    R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM.
  9. RAF/VEGFR Inhibitor

    Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM.
  10. c-Met inhibitor

    AMG-458 is a potent inhibitor of c-Met with an IC50 value of 60nM and displays selectivity against VEGFR2.
  11. EGFR, HER2 and VEGFR inhibitor

    XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4.
  12. C-Met inhibitor

    NVP-BVU972 is a selective MET inhibitor.
  13. EGFR Inhibitor

    AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.
  14. EGFR inhibitor

    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
  15. FGFR/VEGFR2 inhibitor

    LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
  16. c-Met Inhibitor

    EMD-1214063 is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. It binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase.
  17. Itk Inhibitor

    The ITK inhibitor BMS-509744 disrupts several aspects of HIV replication.
  18. PDGFRα/β inhibitor

    CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.
  19. c-Met/VEGFR-2 inhibitor

    E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity.
  20. VEGFR inhibitor

    Apatinib (YN968D1) is a tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2, also known as KDR) that inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue.
  21. 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.
  22. M-CSFR, CSF1R inhibitor

    Ki 20227 is an inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R).
  23. FAK inhibitor

    NVP-TAE226 is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2(IC50=3.5 nM); 10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.
  24. VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor

    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  25. c-Met Inhibitor

    MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
  26. Raf kinase inhibitor

    Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor.
  27. (-)-Catechin gallate is an antioxidant constituent of green tea. At uM concentrations, inhibits VEGF-induced tyrosine phosphorylation.
  28. Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
  29. PKC inhibitor

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
  30. Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor.
  31. multi-targeted tyrosine kinase inhibitor

    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  32. Eph receptor inhibitor

    ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor.
  33. c-MET inhibitor

    LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
  34. TrkA inhibitor

    AZ 23 is a potent and selective tyrosine kinase Trk inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively
  35. Src Inhibitor

    PP1 is a potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl
  36. CSF-1 receptor inhibitor

    Edicotinib is a selective and orally available colony-stimulating factor-1 (CSF-1) receptor inhibitor, and has entered phase IIA clinical trial to study rheumatoid arthritis (RA) despite disease.
  37. EGFR inhibitor

    CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
  38. Lck inhibitor

    AMG-47a is an orally bioavailable potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED50 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
  39. Src Kinase inhibitor

    1-NA-PP1 is a selective inhibitor of v-Src and c-Fyn as well as c-Abl
  40. SRC stimulator

    MCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator.
  41. CDK/JAK2/FLT3 inhibitor

    SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively.
  42. c-Abl/c-Kit/PDGRFβ inhibitor

    Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
  43. VEGFR/PDGFR inhibitor

    TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity.
  44. EGFR Inhibitor

    EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.
  45. ALK inhibitor

    CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
  46. EGFR inhibitor

    CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
  47. Mer Inhibitor

    UNC569 is a novel small-molecule MER inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. UNC569 is the first small-molecule Mer inhibitor. UNC569 inhibited Mer activation and downstream signaling through ERK1/2 and AKT.
  48. Src inhibitor

    PD 166285 is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1).
  49. TrkB inhibitor

    ANA-12 is a TrkB receptor antagonist that demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively.
  50. I3 receptor Antagonist

    KU14R is an antagonist of the pancreatic β-cell atypical imidazoline binding site (putative I3 receptor). KU14R has also been shown to selectively block efaroxan-induced insulin secretion.

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