Protein Tyrosine Kinases

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  1. VEGFR2/Src inhibitor

    TG 100572 is VEGFR2 and Src kinase inhibitor.
  2. Src inhibitor

    CGP77675 is a potent Src kinase inhibitor. CGP77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively).
  3. EGFR inhibitor

    Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
  4. Src inhibitor

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

    ANA-12 is a TrkB receptor antagonist that demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively.
  6. DDR1 receptor inhibitor

    DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with IC50/EC50 of 105 nM/87 nM, 4-fold less potent for DDR2 (IC50= 413 nM).
  7. Dual FLT3/CDK4 inhibitor

    AMG-925 is a potent, selective, and bioavailable FLT3/cyclin-dependent kinase 4 (CDK4) dual kinase inhibitor.
  8. JAK3 inhibitor

    WHI-P 154 is a JAK3 inhibitor with IC50 = 1.8uM. WHI-P 154 also Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro.
  9. dual Lck/Src inhibitor

    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively.
  10. mutil-targeted protein tyrosine kinase inhibitor

    AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
  11. ALK inhibitor

    Lorlatinib (PF-06463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.

  12. FLT3 inhibitor

    G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y).
  13. Mer tyrosine kinase inhibitor

    UNC2881 is a specific Mer tyrosine kinase inhibitor
  14. NUAK kinase inhibitor

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2
  15. Src inhibitor

    A419259 is an apoptosis inducing agent that inhibits Src family kinases (c-Src).
  16. c-Met/VEGFR inhibitor

    Altiratinib is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.
  17. VEGFR inhibitor

    Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.
  18. irreversible EGFR inhibitor

    ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
  19. FGFR1/2/3 inhibitor

    Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity.
  20. EGFR T790M inhibitor

    EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.
  21. c-Met inhibitor

    Volitinib is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase with potential antineoplastic activity.
  22. FGFR1 inhibitor

    ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase).
  23. ALK5 inhibitor

    A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
  24. VEGF and PDGF inhibitor

    Ningetinib Tosylate,also known as CT-053Tosylate and DE-120, is a VEGF and PDGF inhibitor potentially for the treatment of wet age-related macular degeneration. CAS: 1394820-69-9 (free base) 1394820-77-9 (tosylate)
  25. tyrosine kinase inhibitor

    Ningetinib is a multi-kinase inhibitor that inhibits c-Met, VEGFR2/KDR, and Axl with IC50s value of 19, 37, and 11 nM, respectively.
  26. EGFR/HER2 dual inhibitor

    Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
  27. EGFR inhibitor

    Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor.
  28. RTK inhibitor

    Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. CAS: 1058156-90-3 (free base) 1360460-82-7 (HCl)
  29. EGFR inhibitor

    Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).
  30. EGFR inhibitor

    AG-99 is an epidermal growth factor receptor (EGFR) kinase inhibitor with IC50 value of 10 μM.
  31. EGFR inhibitor

    AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells.
  32. VEGFR2 inhibitor

    SU 5205 is a VEGFR2 inhibitor.
  33. VEGFR2 Kinase Inhibitor

    SU-5408, also known as VEGFR2 Kinase Inhibitor I, is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 value of 70 nM.
  34. FGFR inhibitor

    PD166866 is a FGFR1 inhibitor with IC50 value of 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
  35. c-kit inhibitor

    ISCK03 is a potent c-kit inhibitor.
  36. Trk inhibitor

    PF-06737007 is pan tropomyosin-related kinase (Trk) inhibitor.
  37. IRAK4 inhibitor

    AS-2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 value of 21 nM.
  38. IRAK4 inhibitor

    PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4).
  39. ITK inhibitor

    GNE-4997 is a potent and selective ITK inhibitor with Ki value of 0.09 nM.
  40. ITK inhibitor

    PF 06465469 is a potent the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase) inhibitor. It also inhibits BTK.
  41. Itk inhibitor

    GSK-2250665A is a Itk inhibitor with pKi = 9.2, it Exhibits selectivity for Itk over Aurora B kinase and Btk (pIC50 values are 6.4 and 6.5, respectively) and a panel of other kinases. Inhibits IFNγ production in PBMCs.
  42. ITK inhibitor

    CTA 056 is a potent and selective ITK inhibitor (interleukin-2-inducible T-cell kinase inhibitor).
  43. PDGFR inhibitor

    AG1295 is a PDGF receptor specific inhibitor.
  44. cFMS Receptor Inhibitor

    BUN60856, also known as cFMS Receptor Inhibitor II, is a cFMS inhibitor.
  45. VEGFR-2 inhibitor

    Apatinib mesylate(YN968D1 mesylate) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM.

  46. 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.
  47. Raf/VEGFR3 inhibitor

    Sorafenib (Bay 43-9006) is a potent, orally active multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  48. FLT3/AXL inhibitor

    Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
  49. EGFR inhibitor

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
  50. EGFR/PI3K dual inhibitor

    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.

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