EGFR/HER2

Catalog No.Inhibitor Name EGFR/ErbB1HER2/ErbB2ErbB3ErbB4Other
A10362Erlotinib HCl
****
A10422Gefitinib
**
A10514Lapatinib Ditosylate
**
**
*
c-Src
A10141Afatinib
****
**
A10638Neratinib
*
*
KDR,Src
A10211Canertinib
****
***
A11752Lapatinib
**
**
*
c-Src
A10047AG-490
*
*
JAK2
A10242CP-724714
**
A11051Dacomitinib
***
*
*
A10991WZ4002
****
***
A10116Sapitinib
***
***
HDAC,HDAC1,HDAC6
A10246CUDC-101
***
**
A11022AG-1478
***
A10702PD153035 HCl
****
Src,MEK/ERK,Raf
A10706Pelitinib
*
*
c-Abl,FLT1,c-Fms
A10043AEE788
****
***
*
MEK,LCK,VEGFR2
A11209AC480
**
*
*
A10678OSI-420
****
A10990WZ3146
****
A11155AST-1306
****
***
****
A13028Rociletinib
**
A11158Varlitinib
***
****
A13825Icotinib
***
MEK1,Aurora B,LCK
A11236TAK-285
**
**
*
Src,VEGFR,JAK3
A14049WHI-P154
***
A12725PD168393
****
A13755CNX-2006
**
PDGFR
A11949Tyrphostin 9
*
A15940AG-18
*
A15551AZD3759
****
A14985Afatinib Dimaleate
****
**
A13146CL-387785
****
A13044Poziotinib
***
***
**
A13681Osimertinib
**
BLK,ACK1,BRK
A15516AZ5104
****
***
A10992WZ8040
topo II
A10426Genistein
A12448Butein
mTOR
A10210Chrysophanic Acid
A10053Tyrphostin AG 879
*
Trk
A10286Daphnetin
*
PKC, PKA
A11027Irbinitinib (ARRY-380, ONT-380)
****
A11028AV-412
***
*
A11334BIBX 1382
****
*
A12867CGP-52411
*
A13588Tyrphostin AG 183
*
A15509WHI-P180
*
Cdk2
A10612Mubritinib (TAK 165)
****
A16413ARRY-380 (Irbinitinib)
****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  1. (-)-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
  2. 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
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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
  27. 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
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. 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
  40. 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
  41. 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
  42. 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
  43. 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
  44. 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
  45. 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
  46. Cyasterone

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

    Catalog No. A22334
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    inhibitor of EGFR and HER2 oncogenic mutants
    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. Learn More
  48. AG1557

    Catalog No. A22324
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    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. Learn More
  49. Alflutinib

    Catalog No. A22316
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    EGFR inhibitor
    Alflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition. Learn More
  50. (Rac)-JBJ-04-125-02

    Catalog No. A22141
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    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. Learn More

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