Protein Tyrosine Kinases

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  1. 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.
  2. pan-KIT mutant inhibitor

    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
  3. 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.
  4. 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.
  5. FMS kinase inhibitor

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

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

    Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor.
  8. 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.
  9. 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.
  10. VEGF and PDGF inhibitor

    Ningetinib Tosylate,also known as CT-053Tosylate and DE-120, is a VEGF and PDGF inhibitor potentially for the treatment of wet age-related macular degeneration. CAS: 1394820-69-9 (free base) 1394820-77-9 (tosylate)
  11. tyrosine kinase inhibitor

    Ningetinib is a multi-kinase inhibitor that inhibits c-Met, VEGFR2/KDR, and Axl with IC50s value of 19, 37, and 11 nM, respectively.
  12. EGFR/HER2 dual inhibitor

    Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
  13. EGFR inhibitor

    Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor.
  14. RTK inhibitor

    Anlotinib, also known as AL3818, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. CAS: 1058156-90-3 (free base) 1360460-82-7 (HCl)
  15. EGFR inhibitor

    Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM).
  16. EGFR inhibitor

    AG-99 is an epidermal growth factor receptor (EGFR) kinase inhibitor with IC50 value of 10 μM.
  17. EGFR inhibitor

    AG-494 is an inhibitor of epidermal growth factor receptor kinase with an IC50 value of 1 μM in HT-22 cells.
  18. VEGFR2 inhibitor

    SU 5205 is a VEGFR2 inhibitor.
  19. VEGFR2 Kinase Inhibitor

    SU-5408, also known as VEGFR2 Kinase Inhibitor I, is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 value of 70 nM.
  20. FGFR inhibitor

    PD166866 is a FGFR1 inhibitor with IC50 value of 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
  21. c-kit inhibitor

    ISCK03 is a potent c-kit inhibitor.
  22. Trk inhibitor

    PF-06737007 is pan tropomyosin-related kinase (Trk) inhibitor.
  23. IRAK4 inhibitor

    AS-2444697 is a potent and selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 value of 21 nM.
  24. IRAK4 inhibitor

    PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4).
  25. ITK inhibitor

    GNE-4997 is a potent and selective ITK inhibitor with Ki value of 0.09 nM.
  26. ITK inhibitor

    PF 06465469 is a potent the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase) inhibitor. It also inhibits BTK.
  27. Itk inhibitor

    GSK-2250665A is a Itk inhibitor with pKi = 9.2, it Exhibits selectivity for Itk over Aurora B kinase and Btk (pIC50 values are 6.4 and 6.5, respectively) and a panel of other kinases. Inhibits IFNγ production in PBMCs.
  28. ITK inhibitor

    CTA 056 is a potent and selective ITK inhibitor (interleukin-2-inducible T-cell kinase inhibitor).
  29. PDGFR inhibitor

    AG1295 is a PDGF receptor specific inhibitor.
  30. cFMS Receptor Inhibitor

    BUN60856, also known as cFMS Receptor Inhibitor II, is a cFMS inhibitor.
  31. VEGFR-2 inhibitor

    Apatinib mesylate(YN968D1 mesylate) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM.

  32. multi-targeted tyrosine kinase inhibitor

    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  33. Raf/VEGFR3 inhibitor

    Sorafenib (Bay 43-9006) is a potent, orally active multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  34. multi-targeted receptor tyrosine kinase inhibitor

    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
  35. ALK inhibitor

    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively.
  36. EGFR inhibitor

    Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
  37. FLT3/AXL inhibitor

    Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
  38. EGFR inhibitor

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
  39. EGFR/PI3K dual inhibitor

    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.
  40. c-Met inhibitor

    JNJ-38877618 is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively.
  41. EGFR inhibitor

    RG14620 is an EGFR inhibitor with an IC50 of 3 μM.
  42. c-Met inhibitor

    Glumetinib (SCC244) is a potent and highly selective c-Met kinase inhibitor with an IC50 of 0.42 nM. Glumetinib shows antitumor activity and a superior safety margin.
  43. EGFR inhibitor

    AG555 is a potent epidermal growth factor receptor (EGFR) kinase inhibitor.
  44. CSF-1R inhibitor

    TE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
  45. c-FMS inhibitor

    c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively.
  46. c-KIT inhibitor

    c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
  47. ALK inhibitor

    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.
  48. c-KIT T670I mutant inhibitor

    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
  49. FLT3 inhibitor

    FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia.
  50. Mer tyrosine kinase inhibitor

    UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).

Items 351-400 of 553

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