Protein Tyrosine Kinases

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  1. EGFR/HER2 dual inhibitor

    Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 s of 13 and 38 nM, respectively.
  2. triplex matriptase inhibitor

    SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.
  3. Src/c-Abl inhibitor

    1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
  4. DDR1 receptor tyrosine kinase inhibitor

    DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
  5. FGFR3 inhibitor

    Dovitinib(CHIR-258; TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) with an IC50 of 5 nM.
  6. VEGFR inhibitor

    Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  7. VEGFR2/KDR inhibitor

    Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.
  8. tyrosine kinase inhibitor

    Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
  9. EGFR, HER2 and HER4 inhibitor

    Epertinib hydrochloride is a potent, orally active, 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.
  10. dual c-Met/Ron inhibitor

    MK8033 Hcl 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.
  11. VEGFR-2/FGFR inhibitor

    CP-547632 hydrochloride is a well-tolerated, orally-bioavailable inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively.
  12. EGFR inhibitor

    BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFR.
  13. RAK-4/IRAK-1/TAK1 inhibitor

    HS-243 is an inhibitor of transforming growth factor-?beta kinase. HS-243 can be used in treatment of cancer, malaria, inflammatory and other TAK1-?mediated diseases.
  14. Src inhibitor

    DGY-06-116 is an irreversible covalent, selective Src inhibitor.
  15. FGFR-1, PDGFR-β, EGFR inhibitor

    PD089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR with IC50 of 0.15 µM, 1.76 µM, and 5.47 µM, respectively.

  16. AXL kinase inhibitor

    DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM.
  17. EGFR inhibitor

    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M.
  18. inhibitor of Activin receptor-like kinase (ALK2) mutant R206H

    ALK2-IN-1 (BLU-782) is a potent and selective inhibitor of Activin receptor-like kinase (ALK2) mutant R206H with binding IC50 of <10 nM.
  19. pan-PIM/FLT3 inhibitor

    SEL24-B489 is a potent, type I, orally active dual inhibitor of PIM kinases and FLT3-ITD. It exhibits high affinity for PIM family members, with Kd values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3, making it a promising candidate for targeted cancer therapy.
  20. EGFR inhibitor

    Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM.
  21. Axl/Mer inhibitor

    ONO-7475 is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively.
  22. EGFR inhibitor

    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations.
  23. EGFR/HER2 oncogenic mutants inhibitor

    Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  24. EGFR tyrosine kinase inhibitor

    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM.
  25. FGFR1 inhibitor

    Ferulic acid sodium is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
  26. EGFR inhibitor

    Alflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.
  27. TACC3 inhibitor

    BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM.
  28. EGFR inhibitor

    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
  29. FLK-1 (VEGFR-2) / HER2 inhibitor

    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
  30. dual c-Met/RON inhibitor

    SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively.
  31. c-Met inhibitor

    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
  32. VEGFR-3 (Flt-4) inhibitor

    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase.
  33. IRAK4 inhibitor

    IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM.
  34. EGFT/HER2 inhibitor

    Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
  35. VEGFR-2 inhibitor

    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
  36. Src kinase inhibitor

    7-Hydroxychromone is a Src kinase inhibitor with an IC50 of <300 μM.
  37. VEGFR2 and EGFR signalling inhibitor

    ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
  38. FGFR inhibitor

    NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
  39. pan-Trk inhibitor

    PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
  40. ALK5 inhibitor

    TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.
  41. EGFR inhibitor

    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae).
  42. VEGFR2 inhibitor

    ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
  43. dual inhibitor for c-Met and EGFR

    Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
  44. FGFR inhibitor

    2,5-Dihydroxybenzoic acid is a derivative of benzoic and a powerful inhibitor of fibroblast growth factors.
  45. MET/VEGFR2/MER inhibitor

    XL092 is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values in cell-based assays of 15, 1.6, 3.4, and 7.2 nM respectively.
  46. IRAK4/FLT3 inhibitor

    Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation.
  47. FGFR/PDGFR/IGF-1R inhibitor

    SU4984 is a cell-permeable, reversible, and ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1 (FGFR1; IC50 = 10-20 &mu;M).

  48. PDGFR inhibitor

    Seralutinibm, also known as PK-10571 and GB002, is a Inhaled Pdgfr Kinase Inhibitor.
  49. FGFR inhibitor

    E-7090 is a fibroblast growth factor receptor inhibitor potentially for the treatment of solid tumors.
  50. multi-kinase inhibitor

    Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.

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