Protein Tyrosine Kinases

Items 901-950 of 1870

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  1. dual c-Met/RON inhibitor

    SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively.
  2. c-Met inhibitor

    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
  3. VEGFR-3 (Flt-4) inhibitor

    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase.
  4. IRAK4 inhibitor

    IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM.
  5. EGFT/HER2 inhibitor

    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  6. VEGFR-2 inhibitor

    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
  7. Src kinase inhibitor

    7-Hydroxychromone is a Src kinase inhibitor with an IC50 of <300 μM.
  8. VEGFR2 and EGFR signalling inhibitor

    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  9. FGFR inhibitor

    NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
  10. pan-Trk inhibitor

    PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
  11. ALK5 inhibitor

    TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.
  12. EGFR inhibitor

    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae).
  13. VEGFR2 inhibitor

    ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
  14. dual inhibitor for c-Met and EGFR

    Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
  15. FGFR inhibitor

    2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors.
  16. MET/VEGFR2/MER inhibitor

    XL092 is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values in cell-based assays of 15, 1.6, 3.4, and 7.2 nM respectively.
  17. IRAK4/FLT3 inhibitor

    Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.
  18. FGFR/PDGFR/IGF-1R inhibitor

    SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 &mu;M).

  19. PDGFR inhibitor

    Seralutinibm, also known as PK-10571 and GB002, is a Inhaled Pdgfr Kinase Inhibitor.
  20. FGFR inhibitor

    E-7090 is a fibroblast growth factor receptor inhibitor potentially for the treatment of solid tumors.
  21. PDGFRα/PDGFRβ inhbitor

    JNJ 10198409 is a potent platelet-derived growth factor receptor (PDGFR) inhibitor (IC50 values are 4.2 and 45 nM for PDGFRβ and PDGFRα, respectively). Also inhibits c-Abl, Lck, c-Src and Fyn kinases (IC50 values are 22, 100, 185 and 378 nM respectively).
  22. EGFR inhibitor

    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
  23. T790M-Containing EGFR Mutants inhibitor

    PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants.
  24. 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.
  25. 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.
  26. EGFR antagonist

    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
  27. 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.
  28. 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
  29. EGFR/HER2 inhibitor

    Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.
  30. TrkA agonist

    Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
  31. VEGFR2 inhibitor

    VEGFR-2-IN-5 is a VEGFR2 inhibitor extracted from patent WO2013055780A1, Page 31.
  32. 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.
  33. 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.
  34. Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog.
  35. 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.
  36. 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.
  37. 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.
  38. VEGFR2 inhibitor

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

    c-Fms-IN-1 is a FMS kinase inhibitor with an IC50 of 0.0008 μM.
  40. 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.
  41. 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.
  42. dual FLT3/Aurora kinase inhibitor

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

    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  44. 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.
  45. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitic C virus and intracellular bacterial infections.
  46. 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).
  47. 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.
  48. GENZ-882706(Raceme) is the racemate of GENZ-882706.
  49. 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.
  50. 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.

Items 901-950 of 1870

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