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. (-)-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. Neratinib (HKI-272)

    Catalog No. A10638
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    HER2 inhibitor
    Neratinib (HKI-272) is a tyrosine kinase inhibitor. Learn More
  4. 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
  5. 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
  6. 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
  7. WZ4002

    Catalog No. A10991
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    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. Learn More
  8. 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
  9. 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
  10. Lapatinib Ditosylate

    Catalog No. A10514
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    HER2 inhibitor
    Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Learn More
  11. 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
  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. CUDC-101

    Catalog No. A10246
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    HDAC inhibitor
    CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2. Learn More
  14. WZ8040

    Catalog No. A10992
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    EGFR Inhibitor
    WZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation. Learn More
  15. WZ3146

    Catalog No. A10990
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    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
  16. PD153035 (HCl salt)

    Catalog No. A10702
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    EGFR inhibitor
    PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. Learn More
  17. 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
  18. BMS 599626 (AC480)

    Catalog No. A11209
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    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
  19. Arry-380 analog

    Catalog No. A11027
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    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. Learn More
  20. 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
  21. 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
  22. AEE788

    Catalog No. A10043
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    EGFR inhibitor
    AEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2. Learn More
  23. Chrysophanic acid (Chrysophanol)

    Catalog No. A10210
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    EGFR inhibitor
    Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. Learn More
  24. 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
  25. XL647 (Tesevatinib)

    Catalog No. A11057
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    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. Learn More
  26. AST-1306

    Catalog No. A11155
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    EGFR Inhibitor
    AST-1306, a novel anilino-quinazoline compound, inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. Learn More
  27. Daphnetin

    Catalog No. A10286
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    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. Learn More
  28. Mubritinib (TAK 165)

    Catalog No. A10612
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    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. Learn More
  29. 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
  30. 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
  31. 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
  32. TAK-285

    Catalog No. A11236
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    HER2/EGFR inhibitor
    TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1] Learn More
  33. AST-6

    Catalog No. A10062
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    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 Learn More
  34. Tyrphostin AG 879

    Catalog No. A10053
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    HER2 inhibitor
    Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. Learn More
  35. 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
  36. BIBX 1382

    Catalog No. A11334
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    EGFR inhibitor
    BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR. Learn More
  37. AG-17

    Catalog No. A11949
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    EGFR inhibitor
    AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431. Learn More
  38. Butein

    Catalog No. A12448
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    Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. Learn More
  39. 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
  40. 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
  41. CGP-52411

    Catalog No. A12867
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    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
  42. ARRY-543 (Varlitinib, ASLAN001)

    Catalog No. A12868
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    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
  43. CO-1686 (Rociletinib, AVL-301)

    Catalog No. A13028
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    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
  44. 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
  45. 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
  46. 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
  47. 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
  48. 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
  49. (-)-Gallocatechin

    Catalog No. A12003
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    (-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells. Learn More
  50. WHI-P 154

    Catalog No. A14049
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    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

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