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EGFR/HER2

Items 1-50 of 493

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  1. A10426
    Genistin (Genistoside)
    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.
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  2. A10043
    AEE788

    EGFR inhibitor

    AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2.
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  3. A10211
    Canertinib (CI-1033)

    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).
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  4. A11158
    ARRY334543 (Varlitinib)

    EGFR inhibitor

    ARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2.
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  5. A11416
    Erlotinib

    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.
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  6. A10422
    Gefitinib (Iressa)

    EGFR Inhibitor

    Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
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  7. A18014
    Afatinib

    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.
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  8. A11022
    AG-1478 (Tyrphostin AG-1478)

    EGFR Inhibitor

    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM.
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  9. A11028
    AV-412

    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.
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  10. A10638
    Neratinib (HKI-272)

    HER2 inhibitor

    Neratinib (HKI-272) is a tyrosine kinase inhibitor.
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  11. A10047
    AG-490

    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.
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  12. A13681
    Osimertinib (AZD-9291)

    EGFR inhibitor

    Osimertinib (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.

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  13. A11752
    Lapatinib (free base)

    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

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  14. A10706
    Pelitinib (EKB-569)

    EGFR inhibitor

    Pelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity.
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  15. A10005
    (-)-Epigallocatechin gallate

    Antioxidant, antiangiogenic, antitumor agent

    (-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea.
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  16. A10141
    (E/Z)-BIBW2992 (E/Z-Afatinib)

    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.
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  17. A10116
    AZD8931 (Sapitinib)

    pan-EGFR/pan-erbB inhibitor

    AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.
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  18. A15955
    DM1-SMCC

    potent EGFR inhibitor

    DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate.
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  19. A11558
    SU-5402

    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).
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  20. A10242
    CP-724714

    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) .
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  21. A11051
    Dacomitinib (PF299804, PF299)

    EGFR inhibitor

    Dacomitinib (PF299804, PF299) is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.

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  22. A13044
    Poziotinib

    EGFR inhibitor

    Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.
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  23. A10362
    Erlotinib HCl

    EGFR inhibitor

    Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
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  24. A10678
    OSI-420

    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 .
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  25. A10053
    Tyrphostin AG 879

    HER2 inhibitor

    Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA.
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  26. A10062
    Allitinib tosylate (AST-1306 TsOH, AST-6)

    EGFR inhibitor

    AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo
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  27. A10210
    Chrysophanic acid (Chrysophanol)

    EGFR inhibitor

    Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway.
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  28. A10246
    CUDC-101

    HDAC inhibitor

    CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2.
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  29. A10286
    Daphnetin

    EGFR, PKA,PKC inhibitor

    Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.
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  30. A10425
    Genistein

    EGFR inhibitor

    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
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  31. A10514
    Lapatinib Ditosylate

    HER2 inhibitor

    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
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  32. A10612
    Mubritinib (TAK 165)

    HER2/ErbB2 inhibitor

    Mubritinib (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5.
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  33. A10702
    PD153035 (HCl salt)

    EGFR inhibitor

    PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR.
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  34. A10990
    WZ3146

    EGFR Inhibitor

    WZ3146 is an inhibitor of EGFR receptor kinase mutants carrying a mutation in an active site gatekeeper residue (T790M) and is much less potent against wild-type EGFR kinase.
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  35. A10991
    WZ4002

    EGFR Inhibitor

    WZ4002 is EGFR inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib.
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  36. A10992
    WZ8040

    EGFR Inhibitor

    WZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation.
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  37. A11027
    Arry-380 analog

    HER2 Inhibitor

    ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.
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  38. A11057
    XL647 (Tesevatinib)

    EGFR, HER2 and VEGFR inhibitor

    XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4.
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  39. A21661
    Almonertinib hydrochloride (HS-10296 hydrochloride)

    EGFR/T790M inhibitor

    HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
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  40. A21664
    BMS-599626

    HER1/HER2 inhibitor

    BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively.
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  41. A21666
    Firmonertinib (AST2818) mesylate

    EGFR inhibitor

    AST2818 mesylate is an EGFR inhibitor.
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  42. A21741
    Nazartinib mesylate

    EGFR inhibitor

    Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
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  43. A21747
    Nazartinib S-enantiomer

    EGFR inhibitor

    Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
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  44. A21756
    Pyrotinib dimaleate

    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.
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  45. A21950
    Epertinib hydrochloride

    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.
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  46. A22046
    BI-4020

    EGFR inhibitor

    BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFR.
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  47. A22103
    PD-089828

    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.

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  48. A22141
    (Rac)-JBJ-04-125-02

    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.
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  49. A22215
    Theliatinib

    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.
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  50. A22232
    Almonertinib

    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.
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Items 1-50 of 493

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  1. Inhibitor 436items
  2. Antagonist 1item
  3. Activator 1item
Target
  1. HDAC 1item
  2. HDAC1 1item
  3. HDAC2 1item
  4. HDAC3 1item
  5. HDAC4 1item
  6. HDAC5 1item
  7. HDAC6 1item
  8. HDAC7 1item
  9. HDAC8 1item
  10. HDAC9 1item
  11. HDAC10 1item
  12. EGFR/ErbB1/HER1 15items
  13. ErbB2/HER2 7items
  14. ErbB4/HER4 1item
  15. JAK2 1item
  16. JAK3 2items
  17. STAT3 1item