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Angiogenesis EGFR

EGFR

The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands.The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4). In many cancer types, mutations affecting EGFR expression or activity could result in cancer.
Cat No. product name
T0078 LapatinibHOT Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor.
T0078L Lapatinib ditosylate monohydrate Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with tra...
T0129 Sanguinarine chloride Sanguinarine chloride, a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).
T0373 ErlotinibHOT Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
T0373L Erlotinib hydrochlorideHOT Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
T1144L Lidocaine Hydrochloride hydrate Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.
T1656 VandetanibHOT Vandetanib is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.
T1737 Genistein Genistein is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplas...
T1761 PD153035 hydrochloride PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, C...
T1773 Afatinib Dimaleate Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EG...
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T2032 WHI-P180 WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
T2035 WHI-P258 WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of ne...
T2041 PD153035 PD153035 hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, ...
T2047 AG-1478 AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
T2055 WS3 WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
T2063 AG18 AG-18 inhibits EGFR with IC50 of 35 μM.
T2106 WS6 WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
T2116 AEE788 AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
T2245 CL-387785 CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50: 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a ...
T2280 Endoxifen Z-isomer Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
T2303 AfatinibHOT Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, res...
T2325 NeratinibHOT Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T2364 Irbinitinib Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
T2369 Rociletinib Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
T2446 KI8751 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2479 Tyrphostin 9 Tyrphostin 9 is an Agricultural acaricide, now superseded. Tyrphostin 9 is firstly designed as an EGFR inhibitor
T2483 Dacomitinib Dacomitinib(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45....
T2490 Osimertinib Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small ...
T2491 AZ5104 AZ5104 is a potent EGFR inhibitor.
T2501 Canertinib dihydrochloride Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
T2600 AG-490 AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn,...
T2642 PD173074 PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold fo...
T2705 Mutant EGFR inhibitor Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M re...
T2851 Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μ...
T2859 Biochanin A Biochanin A is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty...
T2959 Ginsenoside Rh2 Ginsenoside Rh2, an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.
T2995 Chrysophanic Acid Chrysophanic acid is an EGFR/mTOR pathway inhibitor, which can be found in rhubarb, and sorrel.
T3024 Avitinib Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with poten...
T3059 AP26113 Brigatinib is a excellently effective and specific ALK inhibitor( IC50 =0.6 nM).
T3108 CUDC-101 CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
T3192 NS1643 NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
T3402 Ginsenoside Rg3 Ginsenoside Rg3 possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the pr...
T3506 Nazartinib Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex...
T3545 RG 13022 RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).
T3558 EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
T3621 Brigatinib Brigatinib is a highly potent and selective ALK inhibitor.
T3634 Osimertinib mesylateHOT Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).
T3659 AZD3759 AZD3759 is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK w...
Lapatinib HOT
T0078CAS 231277-92-2
Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor.
Lapatinib ditosylate monohydrate
T0078LCAS 388082-78-8
Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with tra...
Sanguinarine chloride
T0129CAS 5578-73-4
Sanguinarine chloride, a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).
Erlotinib HOT
T0373CAS 183321-74-6
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
Erlotinib hydrochloride HOT
T0373LCAS 183319-69-9
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
Lidocaine Hydrochloride hydrate
T1144LCAS 6108-05-0
Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.
Vandetanib HOT
T1656CAS 443913-73-3
Vandetanib is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR.
Genistein
T1737CAS 446-72-0
Genistein is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplas...
PD153035 hydrochloride
T1761CAS 183322-45-4
PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, C...
Afatinib Dimaleate
T1773CAS 850140-73-7
Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EG...
WHI-P154
T1985CAS 211555-04-3
WHI-P154 is a potent JAK3 inhibitor.
WHI-P180
T2032CAS 211555-08-7
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
WHI-P258
T2035CAS 21561-09-1
WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of ne...
PD153035
T2041CAS 153436-54-5
PD153035 hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, ...
AG-1478
T2047CAS 153436-53-4
AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
WS3
T2055CAS 1421227-52-2
WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
AG18
T2063CAS 118409-57-7
AG-18 inhibits EGFR with IC50 of 35 μM.
WS6
T2106CAS 1421227-53-3
WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
AEE788
T2116CAS 497839-62-0
AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
CL-387785
T2245CAS 194423-06-8
CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50: 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a ...
Endoxifen Z-isomer
T2280CAS 112093-28-4
Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
Afatinib HOT
T2303CAS 439081-18-2
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, res...
Neratinib HOT
T2325CAS 698387-09-6
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
Pelitinib
T2327CAS 257933-82-7
Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
Irbinitinib
T2364CAS 937263-43-9
Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
Rociletinib
T2369CAS 1374640-70-6
Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
KI8751
T2446CAS 228559-41-9
KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
Tyrphostin 9
T2479CAS 10537-47-0
Tyrphostin 9 is an Agricultural acaricide, now superseded. Tyrphostin 9 is firstly designed as an EGFR inhibitor
Dacomitinib
T2483CAS 1110813-31-4
Dacomitinib(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45....
Osimertinib
T2490CAS 1421373-65-0
Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small ...
AZ5104
T2491CAS 1421373-98-9
AZ5104 is a potent EGFR inhibitor.
Canertinib dihydrochloride
T2501CAS 289499-45-2
Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
AG-490
T2600CAS 133550-30-8
AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn,...
PD173074
T2642CAS 219580-11-7
PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold fo...
Mutant EGFR inhibitor
T2705CAS 1421373-62-7
Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M re...
Daphnetin
T2851CAS 486-35-1
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μ...
Biochanin A
T2859CAS 491-80-5
Biochanin A is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty...
Ginsenoside Rh2
T2959CAS 78214-33-2
Ginsenoside Rh2, an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.
Chrysophanic Acid
T2995CAS 481-74-3
Chrysophanic acid is an EGFR/mTOR pathway inhibitor, which can be found in rhubarb, and sorrel.
Avitinib
T3024CAS 1557267-42-1
Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with poten...
AP26113
T3059CAS 1197958-12-5
Brigatinib is a excellently effective and specific ALK inhibitor( IC50 =0.6 nM).
CUDC-101
T3108CAS 1012054-59-9
CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
NS1643
T3192CAS 448895-37-2
NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
Ginsenoside Rg3
T3402CAS 14197-60-5
Ginsenoside Rg3 possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the pr...
Nazartinib
T3506CAS 1508250-71-2
Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex...
RG 13022
T3545CAS 136831-48-6
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).
EBE-A22
T3558CAS 229476-53-3
EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
Brigatinib
T3621CAS 1197953-54-0
Brigatinib is a highly potent and selective ALK inhibitor.
Osimertinib mesylate HOT
T3634CAS 1421373-66-1
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)).
AZD3759
T3659CAS 1626387-80-1
AZD3759 is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK w...