Protein Tyrosine Kinases

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  1. c-Met Inhibitor

    EMD-1214063 is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. It binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase.
  2. multi-kinase inhibitor

    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.
  3. VEGFR/EGFR Inhibitor

    BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.
  4. multi-kinase inhibitor

    Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  5. Lck inhibitor

    A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
  6. EGFR inhibitor

    BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR.
  7. EGFR inhibitor

    Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
  8. c-Met/VEGFR-2 inhibitor

    E7050 (also known as golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity.
  9. ITK inhibitor

    ITK inhibitor is a potent ITK inhibitor.
  10. IRAK-4 inhibitor

    IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
  11. interleukin-1 receptor associated kinase inhibitor

    IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .
  12. IRAK4 inhibitor

    IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
  13. IRAK inhibitor

    IRAK-IN-6, also known as IRAK inhibitor 6, is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NF-kB and MAPK pathways, which are critical for the production of inflammatory cytokines.
  14. Src inhibitor

    KX2-391 2Hcl is the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
  15. 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.
  16. VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor

    Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.
  17. multi-targeted receptor tyrosine kinases inhibitor

    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  18. VEGFR Inhibitor

    SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), KIT, and fms-like tyrosine kinase 3 (FLT-3)
  19. c-Met Inhibitor

    MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
  20. VEGFR2 inhibitor

    CP-547632 is a novel, potent vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor
  21. ALK inhibitor

    ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.
  22. ALK inhibitor

    ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.

  23. EGFR inhibitor

    AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 μM in the human epidermoid carcinoma cell line A431.
  24. IGF-1R inhibitor

    PQ 401 is a cell-permeable phenylquinolinyl-urea compound that inhibits IGF-1R autophosphorylation.
  25. VEGFR Inhibitor

    ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR).
  26. VEGFR Inhibitor

    ZM 306416 is a VEGF receptor tyrosine kinase inhibitor that inhibits KDR (IC50 = 100 nM) and Flt (IC50 = 2 uM) tyrosine kinases.
  27. FLT3 inhibitor

    TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
  28. Raf kinase inhibitor

    Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor.
  29. IGF1R inhibitor

    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  30. Src-PTK inhibitor

    KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.
  31. VEGFR3 Inhibitor

    SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
  32. CDK/JAK2/FLT3 inhibitor

    SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively.
  33. Tie-2 inhibitor

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

    SKLB610 is a novel potential inhibitor of vascular endothelial growth factor receptor tyrosine kinases inhibits angiogenesis and tumor growth in vivo.
  35. c-Abl/c-Kit/PDGRFβ inhibitor

    Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 a and VEGF in U266 cell line in a time- and dose-dependent manners, so flumatinib mesylate may become a new drug for MM therapy.
  36. VEGFR2/PDGFRβ/EphB4 inhibitor

    JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRβ), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities.
  37. VEGFR/PDGFR inhibitor

    TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with potential antineoplastic activity.
  38. FLT3/CDK inhibitor

    FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.
  39. tyrosine kinase inhibitor

    AG-1288 is a tyrosine kinase inhibitor. Has been shown in human amnion cells (IC50 =21 mM) to block glucocorticoid-induced cytotoxicity, TNFα-induced cytotoxicity, and glucocorticoid-induced COX-2 activity.
  40. EGFR inhibitor

    Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM).
  41. p210 tyrosine kinase inhibitor

    Tyrphostin AG 957 is a potent tyrosine kinase inhibitor. Selectively blocks the tyrosine kinase activity of human p210bcr-abl (Ki = 750 nM) over p140c-abl (Ki = 10 μM).
  42. Alk2 inhibitor

    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
  43. EGFR Inhibitor

    EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.
  44. EGFR inhibitor

    Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
  45. ALK inhibitor

    CEP-28122 is a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.
  46. EGFR inhibitor

    CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer.
  47. Raf inhibitor

    CEP-32496 is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity.
  48. EGFR/HER2/HER4 inhibitor

    Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  49. Mer Inhibitor

    UNC569 is a novel small-molecule MER inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. UNC569 is the first small-molecule Mer inhibitor. UNC569 inhibited Mer activation and downstream signaling through ERK1/2 and AKT.
  50. VEGFR2/Src inhibitor

    TG 100801 is a VEGFR2 targeting prodrug currently in a clinical trial. The active form is TG100572.

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