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$0.00 EGFR/HER2
| Catalog No. | Inhibitor Name | EGFR/ErbB1 | HER2/ErbB2 | ErbB3 | ErbB4 | Other |
|---|---|---|---|---|---|---|
| A10362 | Erlotinib HCl | **** | ||||
| A10422 | Gefitinib | ** | ||||
| A10514 | Lapatinib Ditosylate | ** | ** | * | c-Src | |
| A10141 | Afatinib | **** | ** | |||
| A10638 | Neratinib | * | * | KDR,Src | ||
| A10211 | Canertinib | **** | *** | |||
| A11752 | Lapatinib | ** | ** | * | c-Src | |
| A10047 | AG-490 | * | * | JAK2 | ||
| A10242 | CP-724714 | ** | ||||
| A11051 | Dacomitinib | *** | * | * | ||
| A10991 | WZ4002 | **** | *** | |||
| A10116 | Sapitinib | *** | *** | HDAC,HDAC1,HDAC6 | ||
| A10246 | CUDC-101 | *** | ** | |||
| A11022 | AG-1478 | *** | ||||
| A10702 | PD153035 HCl | **** | Src,MEK/ERK,Raf | |||
| A10706 | Pelitinib | * | * | c-Abl,FLT1,c-Fms | ||
| A10043 | AEE788 | **** | *** | * | MEK,LCK,VEGFR2 | |
| A11209 | AC480 | ** | * | * | ||
| A10678 | OSI-420 | **** | ||||
| A10990 | WZ3146 | **** | ||||
| A11155 | AST-1306 | **** | *** | **** | ||
| A13028 | Rociletinib | ** | ||||
| A11158 | Varlitinib | *** | **** | |||
| A13825 | Icotinib | *** | MEK1,Aurora B,LCK | |||
| A11236 | TAK-285 | ** | ** | * | Src,VEGFR,JAK3 | |
| A14049 | WHI-P154 | *** | ||||
| A12725 | PD168393 | **** | ||||
| A13755 | CNX-2006 | ** | PDGFR | |||
| A11949 | Tyrphostin 9 | * | ||||
| A15940 | AG-18 | * | ||||
| A15551 | AZD3759 | **** | ||||
| A14985 | Afatinib Dimaleate | **** | ** | |||
| A13146 | CL-387785 | **** | ||||
| A13044 | Poziotinib | *** | *** | ** | ||
| A13681 | Osimertinib | ** | BLK,ACK1,BRK | |||
| A15516 | AZ5104 | **** | *** | |||
| A10992 | WZ8040 | topo II | ||||
| A10426 | Genistein | |||||
| A12448 | Butein | mTOR | ||||
| A10210 | Chrysophanic Acid | |||||
| A10053 | Tyrphostin AG 879 | * | Trk | |||
| A10286 | Daphnetin | * | PKC, PKA | |||
| A11027 | Irbinitinib (ARRY-380, ONT-380) | **** | ||||
| A11028 | AV-412 | *** | * | |||
| A11334 | BIBX 1382 | **** | * | |||
| A12867 | CGP-52411 | * | ||||
| A13588 | Tyrphostin AG 183 | * | ||||
| A15509 | WHI-P180 | * | Cdk2 | |||
| A10612 | Mubritinib (TAK 165) | **** | ||||
| A16413 | ARRY-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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(-)-Epigallocatechin gallate
Catalog No. A10005 Antioxidant, antiangiogenic, antitumor agent(-)-Epigallocatechin gallate is a potent anti-oxidant polyphenol flavonoid isolated from green tea. Learn More -
Pelitinib (EKB-569)
Catalog No. A10706 EGFR inhibitorPelitinib (EKB-569) is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Learn More -
Canertinib (CI-1033)
Catalog No. A10211 HER2/ErbB2 inhibitorCanertinib (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 -
BIBW2992 (Afatinib)
Catalog No. A10141 EGFR inhibitorBIBW2992 (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 -
AZD8931 (Sapitinib)
Catalog No. A10116 pan-EGFR/pan-erbB inhibitorAZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling. Learn More -
Gefitinib (Iressa)
Catalog No. A10422 EGFR InhibitorGefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Learn More -
Erlotinib HCl
Catalog No. A10362 EGFR inhibitorErlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). Learn More -
AG-1478 (Tyrphostin AG-1478)
Catalog No. A11022 EGFR InhibitorAG-1478 (Tyrphostin AG-1478) is an inhibitor of EGFR kinase with an IC50 value of 3 nM. Learn More -
OSI-420
Catalog No. A10678 EGFR InhibitorOSI-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 -
CP-724714
Catalog No. A10242 HER2/ErbB2 inhibitorCP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) . Learn More -
AV-412
Catalog No. A11028 EGFR inhibitorAV-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 -
AG-490
Catalog No. A10047 EGFR inhibitorAG 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 -
PF299804 (Dacomitinib, PF299)
Catalog No. A11051 EGFR inhibitorPF299804 is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4. Learn More -
ARRY334543 (Varlitinib)
Catalog No. A11158 EGFR inhibitorARRY334543 is a potent, orally active small molecule inhibitor of EGFR and ErbB-2. Learn More -
Genistin (Genistoside)
Catalog No. A10426 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 -
BMS-690514
Catalog No. A11263 VEGFR/EGFR InhibitorBMS-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 -
Lapatinib (free base)
Catalog No. A11752 Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Learn More -
SU-5402
Catalog No. A11558 VEGFR/FGFR/EGFR inhibitorSU-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 -
PKC 412 (Midostaurin)
Catalog No. A12650 PKC inhibitorPKC 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 -
Icotinib Hydrochloride
Catalog No. A13718 EGFR inhibitorIcotinib 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 -
AZD-9291 (Osimertinib)
Catalog No. A13681 EGFR inhibitorAZD-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 -
Tyrphostin AG 183
Catalog No. A13588 EGFR inhibitorTyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM). Learn More -
CNX-2006
Catalog No. A13755 EGFR inhibitorCNX-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 -
Icotinib
Catalog No. A13825 EGFR inhibitorIcotinib 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 -
Afatinib dimaleate
Catalog No. A14985 EGFR inhibitorAfatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. Learn More -
Erlotinib mesylate
Catalog No. A15081 EGFR inhibitorErlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. Learn More -
Gefitinib hydrochloride
Catalog No. A15093 EGFR InhibitorGefitinib 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 -
Vandetanib trifluoroacetate
Catalog No. A15272 VEGFR/EGFR inhibitorVandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. Learn More -
WHI-P180
Catalog No. A15509 EGFR/Cdk2 inhibitorWHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively. Learn More -
AZ5104
Catalog No. A15516 EGFR inhibitorAZ5104, 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 -
AZD3759
Catalog No. A15551 EGFR inhibitorAZD3759 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 -
ASP8273 (Naquotinib)
Catalog No. A14408 irreversible EGFR inhibitorASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Learn More -
EGF816 (Nazartinib)
Catalog No. A14416 EGFR T790M inhibitorEGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC. Learn More -
AG-18 (Tyrphostin 23)
Catalog No. A15940 EGFR InhibitorAG-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 -
DM1-SMCC
Catalog No. A15955 potent EGFR inhibitorDM1-SMCC is DM1 with a reactive linker SMCC, which can react with antibody to make antibody drug conjugate. Learn More -
Erlotinib
Catalog No. A11416 EGFR inhibitorErlotinib 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 -
Osimertinib dimesylate
Catalog No. A18243 EGFR inhibitorOsimertinib 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 -
Pyrotinib
Catalog No. A19423 EGFR/HER2 dual inhibitorPyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively. Learn More -
TAS6417
Catalog No. A19541 EGFR inhibitorTAS6417 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 -
EGFR-IN-5
Catalog No. A20082 EGFR inhibitorEGFR-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 -
Mutated EGFR-IN-1
Catalog No. A20555 EGFR inhibitorMutated 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 -
PF-06459988
Catalog No. A20608 T790M-Containing EGFR Mutants inhibitorPF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants. Learn More -
NRC-2694
Catalog No. A20643 EGFR antagonistNRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. Learn More -
Naquotinib mesylate
Catalog No. A20762 EGFR inhibitorNaquotinib 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 -
Norcantharidin
Catalog No. A22396 dual inhibitor for c-Met and EGFRNorcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. Learn More -
Cyasterone
Catalog No. A22387 EGFR inhibitorCyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Learn More -
Mobocertinib
Catalog No. A22334 inhibitor of EGFR and HER2 oncogenic mutantsMobocertinib (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 -
AG1557
Catalog No. A22324 EGFR inhibitorAG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194. Learn More -
Alflutinib
Catalog No. A22316 EGFR inhibitorAlflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition. Learn More -
(Rac)-JBJ-04-125-02
Catalog No. A22141 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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