Protein Tyrosine Kinases

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  1. RAF265 (CHIR-265)

    Catalog No. A10773
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    RAF/VEGFR Inhibitor
    RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. Learn More
  2. FIIN-2

    Catalog No. A12357
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    FGFR Inhibitor
    FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively. Learn More
  3. CL-387785 (EKI-785)

    Catalog No. A13146
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    EGFR inhibitor
    CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. Learn More
  4. PD158780

    Catalog No. A16254
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    EGFR inhibitor
    PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor. Learn More
  5. Lapatinib (free base)

    Catalog No. A11752
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    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Learn More
  6. Erlotinib

    Catalog No. A11416
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    EGFR inhibitor
    Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated. Learn More
  7. (-)-Epigallocatechin gallate

    Catalog No. A10005
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    Antioxidant, antiangiogenic, antitumor agent
    (-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea. Learn More
  8. PF299804 (Dacomitinib, PF299)

    Catalog No. A11051
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    EGFR inhibitor
    PF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4. Learn More
  9. AG-1478 (Tyrphostin AG-1478)

    Catalog No. A11022
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    EGFR Inhibitor
    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM. Learn More
  10. Genistin (Genistoside)

    Catalog No. A10426
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    Genistin is an isoflavone found in a number of dietary plants like soy and kudzu. It was shown to stimulate estrogen-dependent breast cancer cell growth in vivo. Learn More
  11. BIBW2992 (Afatinib)

    Catalog No. A10141
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    EGFR inhibitor
    BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. Learn More
  12. OSI-420

    Catalog No. A10678
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    EGFR Inhibitor
    OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain . Learn More
  13. Gefitinib (Iressa)

    Catalog No. A10422
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    EGFR Inhibitor
    Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Learn More
  14. Erlotinib HCl

    Catalog No. A10362
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    EGFR inhibitor
    Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). Learn More
  15. CP-724714

    Catalog No. A10242
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    HER2/ErbB2 inhibitor
    CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) . Learn More
  16. AV-412

    Catalog No. A11028
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    EGFR inhibitor
    AV-412 is an EGFR/HER2 inhibitor that binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis. Learn More
  17. Pelitinib (EKB-569)

    Catalog No. A10706
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    EGFR inhibitor
    Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Learn More
  18. Canertinib (CI-1033)

    Catalog No. A10211
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    HER2/ErbB2 inhibitor
    Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). Learn More
  19. AZD8931 (Sapitinib)

    Catalog No. A10116
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    pan-EGFR/pan-erbB inhibitor
    AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling. Learn More
  20. AG-490

    Catalog No. A10047
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    EGFR inhibitor
    AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src. Learn More
  21. ARRY334543 (Varlitinib)

    Catalog No. A11158
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    EGFR inhibitor
    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2. Learn More
  22. SU-5402

    Catalog No. A11558
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    VEGFR/FGFR/EGFR inhibitor‎
    SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). Learn More
  23. AZD-9291 (Osimertinib)

    Catalog No. A13681
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    EGFR inhibitor
    AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. Learn More
  24. BMS-690514

    Catalog No. A11263
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    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. Learn More
  25. PKC 412 (Midostaurin)

    Catalog No. A12650
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    PKC inhibitor
    PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. Learn More
  26. Icotinib Hydrochloride

    Catalog No. A13718
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    EGFR inhibitor
    Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). Learn More
  27. Tyrphostin AG 183

    Catalog No. A13588
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    EGFR inhibitor
    Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM). Learn More
  28. CNX-2006

    Catalog No. A13755
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    EGFR inhibitor
    CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. Learn More
  29. Icotinib

    Catalog No. A13825
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    EGFR inhibitor
    Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). Learn More
  30. Afatinib dimaleate

    Catalog No. A14985
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    EGFR inhibitor
    Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. Learn More
  31. Erlotinib mesylate

    Catalog No. A15081
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    EGFR inhibitor
    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. Learn More
  32. Gefitinib hydrochloride

    Catalog No. A15093
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    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. Learn More
  33. Vandetanib trifluoroacetate

    Catalog No. A15272
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    VEGFR/EGFR inhibitor
    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. Learn More
  34. WHI-P180

    Catalog No. A15509
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    EGFR/Cdk2 inhibitor
    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively. Learn More
  35. AZ5104

    Catalog No. A15516
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    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. Learn More
  36. AZD3759

    Catalog No. A15551
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    EGFR inhibitor
    AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. Learn More
  37. ASP8273 (Naquotinib)

    Catalog No. A14408
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    irreversible EGFR inhibitor
    ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Learn More
  38. EGF816 (Nazartinib)

    Catalog No. A14416
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    EGFR T790M inhibitor
    EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC. Learn More
  39. AG-18 (Tyrphostin 23)

    Catalog No. A15940
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    EGFR Inhibitor
    AG-18 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 35 ,M in the human epidermoid carcinoma cell line A431. Learn More
  40. DM1-SMCC

    Catalog No. A15955
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    potent EGFR inhibitor
    DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate. Learn More
  41. Osimertinib dimesylate

    Catalog No. A18243
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    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. Learn More
  42. Pyrotinib

    Catalog No. A19423
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    EGFR/HER2 dual inhibitor
    Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. Learn More
  43. TAS6417

    Catalog No. A19541
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    EGFR inhibitor
    TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM. Learn More
  44. EGFR-IN-5

    Catalog No. A20082
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    EGFR inhibitor
    EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. Learn More
  45. Mutated EGFR-IN-1

    Catalog No. A20555
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    EGFR inhibitor
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant. Learn More
  46. PF-06459988

    Catalog No. A20608
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    T790M-Containing EGFR Mutants inhibitor
    PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants. Learn More
  47. NRC-2694

    Catalog No. A20643
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    EGFR antagonist
    NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. Learn More
  48. Naquotinib mesylate

    Catalog No. A20762
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    EGFR inhibitor
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR. Learn More
  49. Norcantharidin

    Catalog No. A22396
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    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. Learn More
  50. Cyasterone

    Catalog No. A22387
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    EGFR inhibitor
    Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Learn More

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