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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Catalog No. Product Name Application Product Information
A16413

ARRY-380 (Irbinitinib)

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.
A14985

Afatinib dimaleate

EGFR inhibitor
Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2.
A14953

Compound 56

EGFR inhibitor
Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR.
A14877

Epidermal Growth Factor Receptor Peptide (985-996)

-
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.
A13673

EGFR Inhibitor

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.
A13044 SALE

Poziotinib

EGFR inhibitor
Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.
A14049

WHI-P 154

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.
A12003 SALE

(-)-Gallocatechin

-
(-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.
A13825

Icotinib

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).
A13755

CNX-2006

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.
A13588

Tyrphostin AG 183

EGFR inhibitor
Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM).
A13681 SALE

AZD-9291 (Osimertinib)

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.
A13718 SALE

Icotinib Hydrochloride

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).
A13028 SALE

CO-1686 (Rociletinib, AVL-301)

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).
A12868

ARRY-543 (Varlitinib, ASLAN001)

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.
A12867

CGP-52411

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.
A12650

PKC 412 (Midostaurin)

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.
A15081

Erlotinib mesylate

EGFR inhibitor
Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
A15093

Gefitinib hydrochloride

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.
A16361

TX1-85-1

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.
A16254

PD158780

EGFR inhibitor
PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor.
A16253

Anlotinib

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.
A16193

EAI045

EGFR inhbitor
EAI045 ia a potent and selective EGFR inhbitor. EAI045 targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
A12725

PD168393

EGFR inhibitor
PD168393 is a potent, cell-permeable, irreversible inhibitor of EGFR with IC50 value of 700 pM.
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.
A15940

AG-18 (Tyrphostin 23)

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.
A13146

CL-387785 (EKI-785)

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.
A14416

EGF816 (Nazartinib)

EGFR T790M inhibitor
EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.
A14408

ASP8273 (Naquotinib)

irreversible EGFR inhibitor
ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
A15551

AZD3759

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.
A15457

D-69491

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.
A15516

AZ5104

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.
A15509

WHI-P180

EGFR/Cdk2 inhibitor
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
A15531

BIBX1382

EGFR inhibitor
BIBX1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 _mu_M) and a range of other related tyrosine kinases (IC50 > 10 _mu_M),
A15272

Vandetanib trifluoroacetate

VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM.
A11558 SALE

SU-5402

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).
A12448

Butein

-
Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor.
A11949

AG-17

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.
A11209 SALE

BMS 599626 (AC480)

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.
A10242 SALE

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) .
A10702

PD153035 (HCl salt)

EGFR inhibitor
PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR.
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.
A10992

WZ8040

EGFR Inhibitor
WZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation.
A10678 SALE

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 .
A11022 SALE

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.
A10514 SALE

Lapatinib Ditosylate

HER2 inhibitor
Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway.
A10362 SALE

Erlotinib HCl

EGFR inhibitor
Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
A10422 SALE

Gefitinib (Iressa)

EGFR Inhibitor
Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
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.
A10116 SALE

AZD8931 (Sapitinib)

pan-EGFR/pan-erbB inhibitor
AZD8931 is an oral, equipotent inhibitor of ErbB1, ErbB2 and ErbB3 receptor signaling.

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