Protein Tyrosine Kinases

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  1. ITK inhibitor

    ITK inhibitor is a potent ITK inhibitor.
  2. c-Met inhibitor

    MK-8033 is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.
  3. IGF1R inhibitor

    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  4. ABL/c-KIT dual kinase inhibitor

    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor.
  5. c-Met inhibitor

    c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity.
  6. EGFR inhibitor

    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively.
  7. EGFR inhibitor

    EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
  8. CSF1R inhibitor

    JNJ-28312141 is an orally active CSF1R inhibitor (Colony-stimulating factor-1 receptor, CRF1R) and also a FLT3 inhibitor. CSF1R is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. JNJ-28312141 represents a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth and skeletal events.
  9. ErbB inhibitor

    ARRY-543 is a novel, oral ErbB family inhibitor that, unlike approved ErbB inhibitors, targets all members of the ErbB family, including ErbB3, either directly or indirectly, and has potential advantages in treating tumors that signal through multiple ErbB family members.
  10. DDR1 inhibitor

    DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.
  11. Insulin levels modulator could be used to treat diabetes.
  12. Tie-2 inhibitor

    AMG-Tie2-1 is a highly potent, non-selective inhibitor of Tie-2 (IC50 <1 nM).
  13. Tyrosine kinase inhibitor

    Tyrosine-kinase inhibitor is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades.
  14. 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).
  15. 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.
  16. 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.
  17. FLT3 inhibitor

    FLT3-IN-2 is potent FLT3 inhibitor.
  18. 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.
  19. multi-targeted tyrosine kinase inhibitor

    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. FLT3 inhibitor

    FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia.
  26. Mer tyrosine kinase inhibitor

    UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).
  27. c-MET kinase inhibitor

    Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
  28. EGFR inhibitor

    EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
  29. EGFR inhibitor

    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
  30. FLT-3 ITD degrader

    PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
  31. FGFR1/DDR2 inhibitor

    FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.
  32. EGFR inhibitor

    DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively.
  33. CSF-1R, c-FMS Type II inhibitor

    c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM.
  34. FMS inhibitor

    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  35. ITK inhibitor

    ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
  36. FGFR/VEGFR inhibitor

    ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
  37. TRK inhibitor

    CH7057288 is a potent and selective TRK inhibitor.
  38. ALK and ROS1 dual inhibitor

    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
  39. pan-Trk inhibitor

    Trk-IN-4 (PF-6683324 isomer) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  40. CSF1R inhibitor

    CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
  41. pan-Trk inhibitor

    Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  42. c-Met inhibitor

    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  43. Axl/VEGFR2 inhibitor

    R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
  44. Tie2 and TrkA/B inhibitor

    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
  45. VEGFR/PDGFR inhibitor

    Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor.
  46. cFMS inhibitor

    c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM.
  47. c-FMS inhibitor

    c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ??10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases.
  48. FLT3 inhibitor

    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively.
  49. Src/Abl kinase inhibitor

    AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
  50. IRAK4 inhibitor

    AZ1495 (compound 28) is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively.

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