Protein Tyrosine Kinases

Items 151-200 of 1870

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  1. EGFR Inhibitor

    AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems.
  2. ALK5 inhibitor

    SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively).
  3. Aurora A/B Kinase inhibitor

    PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
  4. Src inhibitor

    KX2-391 is a novel non-ATP competitive substrate-pocket directed SRC inhibitor.

  5. JAK2 inhibitor

    TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

  6. PI3K Inhibitor

    PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
  7. EGFR Inhibitor

    BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity.
  8. HER2/EGFR inhibitor

    TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1]
  9. FGFR/VEGFR2 inhibitor

    LY2874455 is a novel and potent FGFR/VEGFR Inhibitor.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. EGFR inhibitor

    BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR.
  16. 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.
  17. 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.
  18. ITK inhibitor

    ITK inhibitor is a potent ITK inhibitor.
  19. 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.
  20. interleukin-1 receptor associated kinase inhibitor

    IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .
  21. IRAK modulator

    IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.
  22. IRAK4 inhibitor

    IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.
  23. 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.
  24. IRAK-1-4 inhibitor is a benzimidazole that disrupts the activity of IRAK-1 and -4 with IC50 values of 300 and 200 nM, respectively.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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)
  30. VEGFR Antagonist

    Buflomedil is a vasoactive agent used to treat peripheral vascular disease.
  31. c-Met Inhibitor

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

    CP-547632 is a novel, potent vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor
  33. 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.
  34. 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.

  35. 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.
  36. IGF-1R inhibitor

    PQ 401 is a cell-permeable phenylquinolinyl-urea compound that inhibits IGF-1R autophosphorylation.
  37. 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).
  38. VEGFR Inhibitor

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

    TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
  40. (-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.
  41. Raf kinase inhibitor

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

    AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
  43. Thalidomide-based Cereblon ligand

    Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

  44. Picropodophyllin (AXL1717) is the first targeted oral small-molecule IGF-1 receptor inhibitor with no effect on the insulin receptor.
  45. Src-PTK inhibitor

    KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.
  46. Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
  47. VEGFR3 Inhibitor

    SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
  48. SRC stimulator

    MCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator.
  49. 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.
  50. Tie-2 inhibitor

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

Items 151-200 of 1870

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