Protein Tyrosine Kinases

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  1. ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  2. 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).
  3. 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.
  4. 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.
  5. MNS

    Src/Syk inhibitor

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

    AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
  7. 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).
  8. 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.
  9. 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.
  10. IRS-1/2 inhibitor

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

    BPR1J-097 is a novel small molecule FLT-3 inhibitor with promising in vivo anti-tumour activities.
  12. 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.
  13. FLT3 inhibitor

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

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

    H3B-6527 is a highly selective FGFR4 inhibitor with potent antitumour activity in FGF19 amplified cell lines and mice.
  16. 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.
  17. EGFR inhibitor

    PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
  18. 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.

  19. MET/Axl inhibitor

    Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered.
  20. 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.
  21. RTK inhibitor

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

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

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

    BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM.
  25. 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.
  26. MET inhibitor

    AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor.
  27. HER2 inhibitor

    ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity.
  28. PDGFR inhibitor

    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM.
  29. FGFR inhibitor

    Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
  30. irreversible EGFR inhibitor

    Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
  31. EGFR inhibitor

    Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
  32. SUMO inhibitor

    2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
  33. pan-KIT mutant inhibitor

    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
  34. CSF-1R inhibitor

    AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity), AZD7507 is considered a promising compound as it retained the desired potency and oral pharmacokinetic properties of AZ683.
  35. Lck inhibitor

    KIN001-051 is a potent and selective inhibitor of lck. Lymphocyte-speci?c protein tyrosine kinase (Lck) is a member of the Src-family of non-receptor protein tyrosine kinases and plays a critical role in the initial steps of T cell receptor signaling that trigger the production of cytokines.
  36. FMS kinase inhibitor

    cFMS-IN-2 is a FMS kinase inhibitor with an IC50 of 0.024 μM.
  37. MERTK and FLT3 inhibitor

    MRX-2843 is an orally available small-molecule inhibitor of both MERTK and FLT3.
  38. FGFR inhibitor

    Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor.
  39. ITK and RLK inhibitor

    PRN694 is a highly selective and potent covalent inhibitor of Tec kinases IL-2-inducible T cell kinase (ITK) and resting lymphocyte kinase (RLK). It inhibits Th1 and Th17 differentiation and cytokine production.
  40. IRAK4 inhibitor

    CA-4948 is a potent, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. CA-4948 exhibited the greatest efficacy in four of the five ABC-DLBCL PDX models tested as compared to GBC-DLBCL and ABC/GCB DLBCL PDX models.
  41. VEGFR/c-Met/HGFR inhibitor

    TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
  42. multi-targeted kinase inhibitor

    ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
  43. Src inhibitor

    Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
  44. EGFR/T790M inhibitor

    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
  45. HER1/HER2 inhibitor

    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively.
  46. EGFR inhibitor

    AST2818 mesylate is an EGFR inhibitor.
  47. ALK/MET inhibitor

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

    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
  49. EGFR inhibitor

    Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
  50. EGFR/HER2 dual inhibitor

    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.

Items 701-750 of 1597

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