Protein Tyrosine Kinases

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  1. c-Met inhibitor

    JNJ-38877618 is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively.
  2. EGFR inhibitor

    RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
  3. c-Met inhibitor

    Glumetinib (SCC244) is a potent and highly selective c-Met kinase inhibitor with an IC50 of 0.42 nM. Glumetinib shows antitumor activity and a superior safety margin.
  4. EGFR inhibitor

    AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor.
  5. CSF-1R inhibitor

    TE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
  6. c-FMS inhibitor

    c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively.
  7. c-KIT inhibitor

    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  8. ALK inhibitor

    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.
  9. c-KIT T670I mutant inhibitor

    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
  10. AXL Inhibitor

    TP-0903 is a potent and selective Axl kinase inhibitor with IC50 of 27 nM.
  11. MET/VEGFR-2 inhibitor

    BMS-817378 is a novel prodrug of the dual Met/VEGFR-2 inhibitor BMS-794833.
  12. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  13. Axl inhibitor

    SGI-7079 ,a novel selective Axl inhibitor, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
  14. Bcr-Abl inhibitor

    GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
  15. Dual MER/FLT3 inhibitor

    UNC-2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
  16. c-Met inhibitor

    NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
  17. FLT3/KIT/PDGFRα/PDGFRβ inhibitor

    AC710 is a potent, orally active, and selective platelet-derived growth factor receptor-family kinase inhibitor with potential anticancer activity.
  18. EGFR Inhibitor

    AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431.
  19. FGFR2 Inhibitor

    Alofanib is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity.
  20. FGFR inhibitor

    Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity.
  21. TRK inhibitor

    Larotrectinib (LOXO-101, ARRY-470) is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC.

  22. Brk inhibitor

    Tilfrinib is a potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 3.15 nM).
  23. ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
  24. EGFR inhbitor

    EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
  25. ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  26. neuropilin-1/VEGF-A inhibitor

    EG00229 is the first small molecule inhibitors of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells).
  27. TrkA inhibitor

    GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.
  28. TRK inhibitor

    LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
  29. MNS

    Src/Syk inhibitor

    MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases.
  30. Src inhibitor

    AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
  31. Src inhibitor

    T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
  32. Src inhibitor

    T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
  33. FLT3/KIT/PDGFRα/PDGFRβ inhibitor

    AC710 Mesylate is a potent, selective PDGFR-family kinases inhibitor with Kd values of 0.6 nM/1.0 nM/1.3 nM/1.0 nM for FLT3/KIT/PDGFRα/PDGFRβ respectively.
  34. IRS-1/2 inhibitor

    NT157 is a selective inhibitor of IRS-1/2.
  35. FLT3 inhibitor

    BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities.
  36. FLT3 inhibitor

    FLT3-IN-1 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
  37. FLT3 inhibitor

    FLT3-IN-2 is potent FLT3 inhibitor.
  38. FGFR4 inhibitor

    FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM.
  39. FGFR4 inhibitor

    H3B-6527 is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
  40. EGFR inhibitor

    Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.
  41. EGFR inhibitor

    PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
  42. c-Met inhibitor

    SCR-1481B1 is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.

  43. MET/Axl inhibitor

    Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered.
  44. multi-kinase inhibitor

    Flumatinib is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRbeta and c-Kit respectively.
  45. RTK inhibitor

    Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth.
  46. dual Bcr-Abl/Lyn inhibitor

    Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.
  47. ALK/EGFR inhibitor

    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
  48. VEGFR2 inhibitor

    BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.
  49. Her3 (ErbB3) ligand

    TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function.
  50. MET inhibitor

    AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor.

Items 251-300 of 1597

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