Protein Tyrosine Kinases

Items 1001-1050 of 1870

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Citations
  1. TAM inhibitor

    RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain.
  2. FMS inhibitor

    c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity.
  3. RTC-5 is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
  4. ITK inhibitor

    ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM.
  5. FGFR/VEGFR inhibitor

    ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively.
  6. pan-TAM receptor inhibitor

    RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively.
  7. TAM inhibitor

    TAM-IN-2 is a TAM inhibitor extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904.
  8. TRK inhibitor

    CH7057288 is a potent and selective TRK inhibitor.
  9. TKI inhibitor

    Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor (TKI), with IC50s of 0.6 nM, <2.5 nM for TRKA and TRKC respectively.
  10. pan-KIT mutant inhibitor

    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
  11. F-1

    ALK and ROS1 dual inhibitor

    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
  12. pan-Trk inhibitor

    Trk-IN-4 (PF-6683324 isomer) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  13. CSF1R inhibitor

    CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
  14. pan-Trk inhibitor

    Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  15. c-Met inhibitor

    c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
  16. RET/RAF/SRC/S6K inhibitor

    AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
  17. FGFR1-4/CSF1R inhibitor

    PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
  18. Axl/VEGFR2 inhibitor

    R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
  19. Tie2 and TrkA/B inhibitor

    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
  20. HER2 inhibitor

    TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM.
  21. VEGFR-2 inhibitor

    Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
  22. VEGFR/PDGFR inhibitor

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

    c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM.
  24. SDZ281-977 is an antiproliferative agent. It acts by binding to the ??colchicine binding site?? on tubulin and inhibiting tubulin polymerization in vitro.
  25. 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.
  26. EGFR/HER2 dual inhibitor

    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. Kaempferitrin is a naturally-occurring kaempferol glycoside which can be isolated from the leaves of various plants used in traditional herbal medicine.
  32. 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).
  33. 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.
  34. EGFR inhibitor

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

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

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

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

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

    AST487 is a Ret kinase inhibitor/FLT3 inhibitor with IC50 of 0.88 uM for Ret.
  40. 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.

  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. EGFR inhibitor

    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
  46. 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.
  47. 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.
  48. Lck Inhibitor

    TC-S 7003 is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.
  49. 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 .
  50. 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.

Items 1001-1050 of 1870

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