Protein Tyrosine Kinases

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  1. FGFR 1/2/3/4 inhibitor

    ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity.
  2. TRPM8 inhibitor

    BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
  3. EGFR inhibitor

    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
  4. FLT3 inhibitor

    HM-43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations
  5. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  6. VEGFR2 inhibitor

    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.
  7. PDGFR/VEGFR/Src inhibitor

    PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC50 values.
  8. ALK/TRKA/TRKB/TRKC inhibitor

    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7?nM for wild-type recombinant ALK kinase.
  9. ALK inhibitor

    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  10. ATP-competitive multitargeted kinase inhibitor

    Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively.
  11. Raf/EGFR inhibitor

    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
  12. VEGFR2 inhibitor

    BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
  13. FMS kinase inhibitor

    c-Fms-IN-1 is a FMS kinase inhibitor with an IC50 of 0.0008 μM.
  14. IGF1R inhibitor

    E 804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.
  15. MET inhibitor

    SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays.
  16. dual FLT3/Aurora kinase inhibitor

    CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor.
  17. VEGFR inhibitor

    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  18. EGFR inhibitor

    Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.
  19. VEGFR inhibitor

    AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
  20. EGFR/HER2/HER4 inhibitor

    BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
  21. c-Met/HGFR inhibitor

    TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
  22. MET, AXL/MER, and FGFR1/2/3 inhibitor

    S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
  23. TACC3 inhibitor

    KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
  24. Raf/VEGFR3 inhibitor

    Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  25. Raf/VEGFR3 inhibitor

    Sorafenib D4 (Bay 43-9006 D4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  26. multi-targeted tyrosine kinase inhibitor

    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret.
  27. KIT and PDGFRA inhibitor

    Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively.
  28. KIT and PDGFRA switch-control inhibitor

    Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor.
  29. 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.
  30. EGFR inhibitor

    TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
  31. IRAK4 inhibitor

    IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM.
  32. type II PDGFRα kinase inhibitor

    PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
  33. ALK/MET inhibitor

    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  34. ALK5/ALK4 inhibitor

    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  35. FLT3/BTK inhibitor

    CG-806 is an orally active, potent and non-covalent pan-FLT3/pan-BTK inhibitor with an IC50 of 0.08 μM for FLT3. CG-806 has an IC50 of 11 nM against FLT3 wild type (WT)-transfected Ba/F3 cells.
  36. ROS1/TRK inhibitor

    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor.
  37. c-Src inhibitor

    UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
  38. SRC inhibitor

    CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
  39. ALK/ ROS1 dual inhibitor

    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
  40. FLT3 inhibitor

    FF-10101 is a potent FLT3 inhibitor extracted from patent WO2015056683A1, compound example A. FF-10101 is a novel irreversible FLT3 inhibitor with ic50 of 0.20 nM and 0.16 nM for FLT3 (WT) and FLT3(D835Y), respectively.

  41. EGFR inhibitor

    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
  42. c-Src inhibitor

    KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
  43. FLT3 inhibitor

    FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.
  44. ALK inhibitor

    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
  45. KDR/VEGFR2 inhibitor

    KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
  46. Src-family kinase Fgr inhibitor

    TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM.
  47. FGFR inhibitor

    Pemigatinib is a selective FGFR inhibitor in development for the treatment of patients with cholangiocarcinoma.
  48. Src inhibitor

    WEHI-345 analog is a Src inhibitor, extracted from patent WO/2012003544A1, compound example 71.
  49. AXL/c-Met inhibitor

    CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
  50. PDGFRα/β inhibitor

    GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively.

Items 801-850 of 1597

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