EGFR/HER2

Inhibitory Selectivity
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. AV412

    Catalog No. A15460
    EGFR inhibitor
    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M?and ErbB2, respectively. Learn More
  2. Erlotinib mesylate

    Catalog No. A15081
    EGFR inhibitor
    Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. Learn More
  3. Afatinib dimaleate

    Catalog No. A14985
    EGFR inhibitor
    Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. Learn More
  4. Compound 56

    Catalog No. A14953
    EGFR inhibitor
    Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR. Learn More
  5. Epidermal Growth Factor Receptor Peptide (985-996) exists on the cell surface and is activated by the binding of its specific ligands, including epidermal growth factor and transforming growth factor. Learn More
  6. EGFR Inhibitor

    Catalog No. A13673
    EGFR Inhibitor
    EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells. Learn More
  7. Poziotinib

    Catalog No. A13044
    EGFR inhibitor
    Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. Learn More
  8. WHI-P 154

    Catalog No. A14049
    JAK3 inhibitor
    WHI-P 154 is a JAK3 inhibitor with IC50 = 1.8uM. WHI-P 154 also Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. Learn More
  9. (-)-Gallocatechin

    Catalog No. A12003
    (-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells. Learn More
  10. Icotinib

    Catalog No. A13825
    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
  11. CNX-2006

    Catalog No. A13755
    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
  12. Tyrphostin AG 183

    Catalog No. A13588
    EGFR inhibitor
    Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM). Learn More
  13. AZD-9291 (Osimertinib)

    Catalog No. A13681
    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
  14. Icotinib Hydrochloride

    Catalog No. A13718
    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
  15. EGFR inhibitor
    CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). Learn More
  16. ErbB inhibitor
    ARRY-543 is a novel, oral ErbB family inhibitor that, unlike approved ErbB inhibitors, targets all members of the ErbB family, including ErbB3, either directly or indirectly, and has potential advantages in treating tumors that signal through multiple ErbB family members. Learn More
  17. CGP-52411

    Catalog No. A12867
    EGFR inhibitor
    CGP-52411 is a slective inhibitor of the epidermal growth factor receptor (EGFR) (IC50 = 0.3 μM in vitro). Also inhibits and reverses the formation of Aβ42 fibers associated with Alzheimer's disease. Learn More
  18. PKC 412 (Midostaurin)

    Catalog No. A12650
    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
  19. Gefitinib hydrochloride

    Catalog No. A15093
    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
  20. VEGFR/EGFR inhibitor
    Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. Learn More
  21. AG-1517

    Catalog No. A13001
    EGFR inhibitor
    AG 1517 is a potent and selective ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR. Learn More
  22. Erlotinib

    Catalog No. A11416
    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
  23. ARRY-380 (Irbinitinib)

    Catalog No. A16413
    HER2 inhibitor
    ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Learn More
  24. TX1-85-1

    Catalog No. A16361
    Her3 (ErbB3) ligand
    TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function. Learn More
  25. PD158780

    Catalog No. A16254
    EGFR inhibitor
    PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor. Learn More
  26. Anlotinib

    Catalog No. A16253
    EGFR inhibitor
    Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer. Learn More
  27. EAI045

    Catalog No. A16193
    EGFR inhbitor
    EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor. Learn More
  28. PD168393

    Catalog No. A12725
    EGFR inhibitor
    PD168393 is a potent, cell-permeable, irreversible inhibitor of EGFR with IC50 value of 700 pM. Learn More
  29. DM1-SMCC

    Catalog No. A15955
    potent EGFR inhibitor
    DM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate. Learn More
  30. AG-18 (Tyrphostin 23)

    Catalog No. A15940
    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
  31. CL-387785 (EKI-785)

    Catalog No. A13146
    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
  32. EGF816 (Nazartinib)

    Catalog No. A14416
    EGFR T790M inhibitor
    EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC. Learn More
  33. ASP8273 (Naquotinib)

    Catalog No. A14408
    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
  34. AZD3759

    Catalog No. A15551
    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
  35. D-69491

    Catalog No. A15457
    HER2 inhibitor
    D-69491 (SU11464) is a small-molecule HER2 inhibitor, which was under development for the treatment of tumours with high expression of HER2, such as breast, ovarian, lung and pancreatic carcinomas. Learn More
  36. AZ5104

    Catalog No. A15516
    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
  37. WHI-P180

    Catalog No. A15509
    EGFR/Cdk2 inhibitor
    WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively. Learn More
  38. SU-5402

    Catalog No. A11558
    VVEGFR/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
  39. Antioxidant, antiangiogenic, antitumor agent
    (-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea. Learn More
  40. BMS 599626 (AC480)

    Catalog No. A11209
    EGFR Inhibitor
    BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity. Learn More
  41. CP-724714

    Catalog No. A10242
    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
  42. PD153035 (HCl salt)

    Catalog No. A10702
    EGFR inhibitor
    PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. Learn More
  43. WZ3146

    Catalog No. A10990
    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. Learn More
  44. WZ8040

    Catalog No. A10992
    EGFR Inhibitor
    WZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation. Learn More
  45. CUDC-101

    Catalog No. A10246
    HDAC inhibitor
    CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2. Learn More
  46. OSI-420

    Catalog No. A10678
    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
  47. EGFR Inhibitor
    AG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM. Learn More
  48. Lapatinib Ditosylate

    Catalog No. A10514
    HER2 inhibitor
    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Learn More
  49. Erlotinib HCl

    Catalog No. A10362
    EGFR inhibitor
    Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). Learn More
  50. Gefitinib (Iressa)

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

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