Protein Tyrosine Kinases

Items 501-550 of 1870

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  1. VEGFR/PDGFR inhibitor

    Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor.
  2. cFMS inhibitor

    c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM.
  3. SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
  4. c-FMS inhibitor

    c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ??10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases.
  5. EGFR/HER2 dual inhibitor

    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  6. FGFR4 inhibitor

    Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity.
  7. FLT3 inhibitor

    BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively.
  8. TrkB/TrkC neurotrophin receptor activator

    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  9. Src/Abl kinase inhibitor

    AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
  10. Kaempferitrin is a naturally-occurring kaempferol glycoside which can be isolated from the leaves of various plants used in traditional herbal medicine.
  11. Rhoifolin is a chemical compound. It is a flavone, a type of flavonoid isolated from Boehmeria nivea, China grass or ramie (leaf), from Citrus limon, Canton lemon (leaf), from Citrus x aurantium, the bigarade or bitter orange (plant), from Citrus x paradisi, the grapefruit (leaf), from Ononis campestris, the cammock (shoot) and from Sabal serratula, the serenoa or sabal fruit (plant).
  12. Epidermal Growth Factor Receptor Peptide (985-996) exists on the cell surface and is activated by the binding of its specific ligands, including epidermal growth factor and transforming growth factor.
  13. EGFR inhibitor

    Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.
  14. EGFR inhibitor

    Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
  15. Ack1 (TNK2) inhibitor

    AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.
  16. ALK inhibitor

    ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
  17. ALK inhibitor

    ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
  18. RET kinase inhibitor

    AST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
  19. FMS inhibitor

    c-Fms-IN-3 is a potent, orally active and small-molecule inhibitor of FMS kinase with IC50 value of 0.8 nM.

  20. c-Met inhibitor

    c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
  21. Src inhibitor

    Dasatinib hydrochloride is a potent and dual Abl/ Src inhibitor IC50 of <1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM.
  22. C-Kit/PDGFR inhibitor

    DCC-2618 is a small molecule inhibitor of c-Kit and PDGFR with IC50s of 6 nM/30 nM/13 nM for c-Kit/PDGFRα/PDGFRβ respectively.
  23. VEGFR/FGFR Inhibitor

    E-3810 is a potent and selective dual inhibitor of VEGF and FGF receptors with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM and 82.5 nM for VEGFR-1, VEGFR-2, VEGFR-3, FGFR-1 and FGFR-2, respectively.
  24. EGFR inhibitor

    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
  25. EGFR Inhibitor

    Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.
  26. JNK Inhibitor

    JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.
  27. Lck Inhibitor

    TC-S 7003 is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.
  28. Lck inhibitor

    Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively .
  29. ALK inhibitor

    LDK378 dihydrochloride is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
  30. MET inhibitor

    LY2801653 dihydrochloride is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
  31. VEGFR/PDGFRβ/KIT inhibitor

    N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively).
  32. FGFR Inhibitor

    NVP-BGJ398 phosphate is a novel selective, pan-specific FGFR inhibitor with IC50 of 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively; >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn, Kit, Lck, Lyn and Yes.
  33. c-Met Inhibitor

    PF-04217903 methanesulfonate is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).
  34. Tyrosine kinase inhibitor

    Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
  35. 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).
  36. VEGFR2/Src kinase inhibitor

    TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
  37. VEGFr2 inhibitor

    TG 100801 is the prodrug of TG 100572, TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.

  38. c-Kit/VEGFR2/PDGFRβ inhibitor

    Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ.
  39. Tyrosine kinase inhibitor

    Tyrosine-kinase inhibitor is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades.
  40. VEGFR/EGFR inhibitor

    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
  41. VEGFR Inhibitor

    ZM323881 is a potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) with IC50 value of 2 nM.
  42. VGF-derived peptide

    TLQP 21, VGF-derived peptide; spans residues 556-576 of the precursor sequence.
  43. HER2 inhibitor

    D-69491 (SU11464) is a small-molecule HER2 inhibitor, which was under development for the treatment of tumours with high expression of HER2, such as breast, ovarian, lung and pancreatic carcinomas.
  44. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  45. TrkB agonist

    LM22A-4 is a potent tropomyosin-related kinase B (TrkB) agonist (IC50 = 47 nM).
  46. EGFR/Cdk2 inhibitor

    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
  47. ACK1/ALK inhibitor

    KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
  48. EGFR inhibitor

    AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
  49. SRC inhibitor

    SU6656 is a selective inhibitor of Src kinases, Including Src, Yes, Lyn, and Fyn (IC50 = 280, 20, 130, 170 nM, respectively).
  50. FMS/KIT inhibitor

    PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.

Items 501-550 of 1870

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