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$0.00 EGFR/HER2
Inhibitory Selectivity
| 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 -
Neratinib (HKI-272)
Catalog No. A10638 HER2 inhibitorNeratinib (HKI-272) is a tyrosine kinase inhibitor. 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 -
WZ4002
Catalog No. A10991 EGFR InhibitorWZ4002 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 -
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 -
Lapatinib Ditosylate
Catalog No. A10514 HER2 inhibitorLapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. 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 -
CUDC-101
Catalog No. A10246 HDAC inhibitorCUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2. Learn More -
WZ8040
Catalog No. A10992 EGFR InhibitorWZ8040 is a novel EGFR inhibitors that suppress the growth of EGFR-T790M-containing cell lines and inhibit EGFR phosphorylation. Learn More -
WZ3146
Catalog No. A10990 EGFR InhibitorWZ3146 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 -
PD153035 (HCl salt)
Catalog No. A10702 EGFR inhibitorPD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. 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 -
BMS 599626 (AC480)
Catalog No. A11209 EGFR InhibitorBMS 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 -
Arry-380 analog
Catalog No. A11027 HER2 InhibitorARRY-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 -
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 -
AEE788
Catalog No. A10043 EGFR inhibitorAEE788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor that inhibits phosphorylation of the tyrosine kinases of EGFR, HER2 and VEGF2. Learn More -
Chrysophanic acid (Chrysophanol)
Catalog No. A10210 EGFR inhibitorChrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. 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 -
XL647 (Tesevatinib)
Catalog No. A11057 EGFR, HER2 and VEGFR inhibitorXL647 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 -
AST-1306
Catalog No. A11155 EGFR InhibitorAST-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 -
Daphnetin
Catalog No. A10286 EGFR, PKA,PKC inhibitorDaphnetin 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 -
Mubritinib (TAK 165)
Catalog No. A10612 HER2/ErbB2 inhibitorMubritinib (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 -
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 -
TAK-285
Catalog No. A11236 HER2/EGFR inhibitorTAK-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 -
AST-6
Catalog No. A10062 EGFR inhibitorAST-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 -
Tyrphostin AG 879
Catalog No. A10053 HER2 inhibitorTyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. Learn More -
Lapatinib (free base)
Catalog No. A11752 Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Learn More -
BIBX 1382
Catalog No. A11334 EGFR inhibitorBIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR. Learn More -
AG-17
Catalog No. A11949 EGFR inhibitorAG-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 -
Butein
Catalog No. A12448 Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. 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 -
CGP-52411
Catalog No. A12867 EGFR inhibitorCGP-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 -
ARRY-543 (Varlitinib, ASLAN001)
Catalog No. A12868 ErbB inhibitorARRY-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 -
CO-1686 (Rociletinib, AVL-301)
Catalog No. A13028 EGFR inhibitorCO-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 -
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 -
(-)-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 -
WHI-P 154
Catalog No. A14049 JAK3 inhibitorWHI-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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