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Catalog No. Product Name Information Product Use Citations Product Validations
A2018New Panitumumab (anti-EGFR) Panitumumab (anti-EGFR, ABX-EGF) is a recombinant, fully human IgG2 monoclonal antibody that binds to the epidermal growth factor receptor (EGFR).
E0368New DZD9008 DZD9008 is an oral, potent, irreversible, wild type-selective EGFR inhibitor against EGFR or HER2 Exon20ins and other mutations with IC50 ranging from 0.4 nM to 2.1 nM for mutant EGFR.
E0822New AST-1306 AST-1306 (Allitinib) is an orally active and irreversible EGFR, ErbB2 and inhibitor with IC50s of 0.5, 3 and 0.8 nM, respectively.
E0833New O-Demethyl-Gefitinib O-Desmethyl gefitinib, a major active metabolite of gefitinib, is a potent EGFR (ErbB1/HER1) inhibitor, inhibits subcellular EGFR tyrosine kinase through a mechanism similar to that of gefitinib with IC50 values of 36 and 22 nM, respectively. 
S0070 Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
S0151 AG-1557 AG-1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
S0360 EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
S0711 Canertinib dihydrochloride Canertinib (CI-1033, PD-183805, compound 18) dihydrochloride is a potent and irreversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively.
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
Sci Rep, 2017,
BMC Cancer, 2017,
S0736 AG 556 AG 556 is an inhibitor of EGFR kinase autophosphorylation over HER1/2 autophosphorylation.
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Cell Death Dis, 2022, 13(6):524
Front Pharmacol, 2022, 13:807440
Int J Mol Med, 2022, 49(6)84
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Nature, 2022, 603(7900):335-342
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Immunol, 2022, 23(2):251-261
S1019 Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
S1023 Erlotinib (OSI-774) HCl Erlotinib (OSI-774, CP358774, NSC 718781) HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Sci Adv, 2022, 8(4):eabi7711
Neuro Oncol, 2022, noac105
J Cachexia Sarcopenia Muscle, 2022, 10.1002/jcsm.12985
S1025 Gefitinib (ZD1839) Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Mol Cancer, 2022, 21(1):43
Sci Adv, 2022, 8(4):eabi7711
Cell Rep, 2022, 39(4):110721
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x
Breast Cancer Res, 2022, 24(1):18
Mol Cancer Ther, 2022, molcanther.0320.2021
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Cancer Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
S1054 AG99 AG99 (Tyrphostin 46,Tyrphostin A46,Tyrphostin B40) is a potent and selective inhibitor of EGFR.
S1056 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
Genome Med, 2020, 18;12(1):17
PLoS Genet, 2016, 12(9):e1006279
Asian J Androl, 2016, 10.4103/1008-682X
S1079 PD153035 HCl PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 HCl) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
Int J Mol Sci, 2021, 22(8)3945
FEBS Lett, 2021, 595(5):563-576
FEBS Lett, 2021, 10.1002/1873-3468.14032
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
J Exp Med, 2022, 219(4)e20211498
J Headache Pain, 2022, 23(1):25
Mol Neurobiol, 2022, 59(5):3280-3293
S1167 CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Biochem J, 2021, BCJ20210173
Int J Mol Sci, 2020, 22(1)E82
NPJ Breast Cancer, 2020, 6:30
S1170 WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
Aging (Albany NY), 2020, 12(19):19022-19044
S1173 WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).
Cancers (Basel), 2021, 13(16)4133
Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w
Cell Res, 2020, 10.1038/s41422-020-00409-1
S1179 WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
Biochemistry, 2018, 57(8):1369-1379
Nat Commun, 2016, 7:10690
S1194 CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1342 Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Genome Med, 2020, 18;12(1):17
Mol Pharmacol, 2019, 95(5):528-536
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cancer Discov, 2022, 12(1):204-219
Cell Metab, 2022, 34(1):90-105.e7
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x
S2115 RG 13022 RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.
S2150 Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.
Cell Metab, 2022, 34(1):90-105.e7
Mol Cancer Ther, 2022, 21(5):751-761
JCO Precis Oncol, 2022, 6:e2100325
S2185 Allitinib tosylate Allitinib tosylate (AST-1306 TsOH, AST-6) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
Front Cell Dev Biol, 2020, 8:605110
Cell Signal, 2020, 65:109439
Life Sci, 2020, 15;251:117634
S2192 Sapitinib (AZD8931) Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
Cell Rep, 2021, 35(11):109233
Cancer Lett, 2021, 519:328-342
Nature, 2020, 584(7822):608-613
S2205 OSI-420 OSI-420 (DesMethyl Erlotinib, CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
Immunol Res, 2022, 10.1007/s12026-022-09262-3
Hum Cell, 2022, 10.1007/s13577-022-00671-y
J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1166:122554
S2250 (-)-Epigallocatechin Gallate (-)-Epigallocatechin Gallate(EGCG) is the main catechin extraction of green tea that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
Exp Cell Res, 2022, 411(1):113000
Int J Mol Med, 2022, 49(1)11
J Cardiovasc Pharmacol, 2022, 79(5):711-718
S2406 Chrysophanic Acid Chrysophanic Acid (Chrysophanol) a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
Cell Prolif, 2020, e12871
Naunyn Schmiedebergs Arch Pharmacol, 2019, 10.1007/s00210-019-01746-8
S2554 Daphnetin Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.
Sci Rep, 2021, 11(1):11491
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
Int Immunopharmacol, 2019, 72:195-203
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
Mol Oncol, 2022, 10.1002/1878-0261.13229
Int J Biol Sci, 2022, 18(5):2047-2059
Sci Rep, 2022, 12(1):6345
S2728 AG-1478 (Tyrphostin AG-1478) AG-1478 (Tyrphostin AG-1478, NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR. AG-1478 (Tyrphostin AG-1478) inhibits encephalomyocarditis virus (EMCV) and hepatitis c virus (HCV) by targeting phosphatidylinositol 4-kinase IIIα (PI4KA).
J Cell Biol, 2022, 221(7)e202111125
Elife, 2022, 11e69906
Int J Biol Sci, 2022, 18(1):349-359
S2733New AV-412 free base AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.51, 0.79, 2.30, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
Commun Biol, 2021, 4(1):762
S2755 Varlitinib Varlitinib (ARRY334543) is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.
Cell Rep Med, 2022, 3(1):100492
Pharmaceutics, 2019, 11(11)
Pharmaceutics, 2018, 10(3)
S2784 TAK-285 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
Oncotarget, 2020, 11(46):4224-4242
Mol Pharmacol, 2019, 95(5):528-536
Sci Signal, 2018, 11(549)
S2867 WHI-P154 WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.
Sci Rep, 2022, 12(1):7
Am J Transplant, 2021, 21(7):2360-2371
J Med Chem, 2020, 31
S2895 Tyrphostin 9 Tyrphostin 9 (SF 6847, RG-50872) is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.
Cell Rep, 2022, 38(10):110475
S2922 Icotinib (BPI-2009H) Icotinib (BPI-2009H) 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).
Cell Rep Med, 2022, 3(1):100492
Nat Cell Biol, 2019, 21(8):1027-1040
Oncogene, 2017, 36(45):6235-6243
S3759 Norcantharidin Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
S4667 Lidocaine hydrochloride Lidocaine hydrochloride (Lidothesin, Lignocaine, Xyloneural) is an inhibitor of epidermal growth factor receptor (EGFR) and has antiproliferative effect on human tongue cancer cells. Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
Exp Ther Med, 2021, 21(5):424
S5078 Osimertinib mesylate Osimertinib mesylate (AZD9291) is the mesylate form of osimertinib, which is an oral, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) drug.
Nature, 2022, 603(7900):335-342
Sci Transl Med, 2022, 14(638):eabc7480
Mol Cancer, 2022, 21(1):43
S5098 Gefitinib hydrochloride Gefitinib (ZD1839) is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.
Mol Cancer, 2022, 21(1):43
Ther Adv Med Oncol, 2022, 14:17588359221079125
Mol Oncol, 2022, 10.1002/1878-0261.13229
S6509 AG 494 AG-494, a member of the tyrphostin family of tyrosine kinase inhibitors, is a potent inhibitor of EGF receptor autophosphorylation (IC50=1.2 μM) and EGF-dependent cell growth (IC50=6 μM).
S6523 RG14620 RG14620 (Tyrphostin RG14620), an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2/BCRP.
S6525 AG 555 AG-555 (Tyrphostin B46) is an inhibitor of tyrosine kinase, interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.
S6541 MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S6546 PD153035 PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).
Sci Signal, 2022, 15(728):eabj6915
Nature, 2021, 10.1038/s41586-020-03085-8
Int J Mol Sci, 2021, 22(8)3945
S6698 TQB3804 (EGFR-IN-7) TQB3804 (EGFR-IN-7) is a selective and potent EGFR kinase inhibitor with IC50 of 0.46 nM, 0.13 nM, 0.26 nM, 0.19 nM and 1.07 nM for for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, EGFRL858R/T790M and EGFRWT, respectively. TQB3804 (EGFR-IN-7) shows anti-tumor activity.
S6805 Tyrphostin AG-528 Tyrphostin AG-528 (Tyrphostin B66) is a potent inhibitor of epidermal growth factor receptors (EGFR) and ErbB2/HER2 with IC50 of 4.9 μM and 2.1 μM, respectively. Tyrphostin AG-528 exhibits anticancer activity.
S6809 SU5214 SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.
S6813 Mobocertinib (TAK788) Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.
Lung Cancer, 2020, 152:135-142
S6868 Alflutinib (AST2818) mesylate Alflutinib (AST2818, Furmonertinib) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
S6881 JND3229 JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively.
S6897 Epertinib hydrochloride Epertinib hydrochloride (S-222611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4 with IC50 of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride (S-222611 hydrochloride) exhibits antitumor activity.
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S7000 AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
Clin Cancer Res, 2015, 21(1):166-74
Clin Cancer Res, 2014, 20(22):5686-96
Jpn J Clin Oncol, 2014, 44(10):963-8
S7039 PD168393 PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.
J Neurosci Res, 2021, 10.1002/jnr.24909
Int J Biochem Cell Biol, 2019, 115:105578
Theranostics, 2017, 7(3):664-676
S7206 CNX-2006 CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w
Cancer Sci, 2016, 107(4):461-8
S7284 Rociletinib (CO-1686) Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Sci, 2021, 112(9):3784-3795
S7297 Osimertinib (AZD9291) Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
Nature, 2022, 603(7900):335-342
Sci Transl Med, 2022, 14(638):eabc7480
Mol Cancer, 2022, 21(1):43
S7298 AZ5104 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.
J Pharm Biomed Anal, 2020, 177:112871
Clin Cancer Res, 2019, 25(8):2575-2587
Sci Rep, 2019, 9(1):5309
S7358 Poziotinib (HM781-36B) Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
JCO Precis Oncol, 2022, 6:e2100325
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00284-1
S7557 CL-387785 (EKI-785) CL-387785 (EKI-785, WAY-EKI 785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
J Biol Chem, 2017, 292(24):10112-10122
Nature, 2017, 550(7675):270-274
Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789
S7786 Erlotinib (OSI-774) Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Sci Adv, 2022, 8(2):eabh3375
Neuro Oncol, 2022, noac105
J Cachexia Sarcopenia Muscle, 2022, 10.1002/jcsm.12985
S7810 Afatinib (BIBW2992) Dimaleate Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.
Nature, 2022, 603(7900):335-342
Nat Immunol, 2022, 23(2):251-261
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
S7824 Nazartinib (EGF816) Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.
Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001
Transl Oncol, 2019, 12(5):705-713
J Thorac Oncol, 2019, 14(9):1556-1566
S7926 Lifirafenib (BGB-283) Lifirafenib (BGB-283, Beigene-283) potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant.
Nat Commun, 2020, 11(1):3157
Cell Rep, 2020, 31(11):107764
Cell Rep, 2019, 29(3):573-588
S7971 Zorifertinib (AZD3759) Zorifertinib (AZD3759) is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1.
Oncogene, 2022, 10.1038/s41388-022-02256-3
Acta Neuropathol, 2020, 10.1007/s00401-020-02226-7
Clin Cancer Res, 2019, 25(8):2575-2587
S8009 AG-18 AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.
Reproduction, 2016, 151(2):179-85
S8036 Butein Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.
Am J Cancer Res, 2020, 10(11):3721-3736
Oncotarget, 2015, 6(14):12637-53
S8229 Brigatinib (AP26113) Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
NPJ Precis Oncol, 2022, 6(1):11
NPJ Precis Oncol, 2022, 6(1):5
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S8242 EAI045 EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.
Pharmazie, 2018, 73(11):630-634
S8294 Olmutinib (BI 1482694) Olmutinib (BI 1482694) is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor (TKI). Also a potent inhibitor of Bruton's tyrosine kinase.
Ther Adv Med Oncol, 2022, 14:17588359221079125
Cancer Cell, 2019, 10.1016/j.ccell.2019.09.001
Sci Rep, 2019,
S8362 Tucatinib Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity.
Cell Metab, 2022, 34(1):90-105.e7
Breast Cancer (Dove Med Press), 2022, 14:25-39
Cancer Cell, 2021, S1535-6108(21)00284-1
S8412 Naquotinib(ASP8273) Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
Expert Opin Emerg Drugs, 2018, 10.1080/14728214.2018.1558203 Share on FacebookShare on TwitterShare on Google+
S8584 Theliatinib (HMPL-309) Theliatinib (HMPL-309) is a highly potent EGFR inhibitor with Ki value of 0.05 nM against the wild type EGFR and IC50 values of 3 nM and 22 nM against EGFR and EGFR T790M/L858R mutant. It demonstrats 50 fold greater selectivity for EGFR compared to 72 other kinases.
S8724 Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
Cancer Res Treat, 2021, 10.4143/crt.2021.385
J Thorac Oncol, 2019, 14(9):1556-1566
Mol Cancer Ther, 2018, 17(10):2257-2265
S8741 Avitinib (AC0010) Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity.
S8814 TAS6417 TAS6417 (CLN-081, TPC-064) is a novel EGFR inhibitor that targets EGFR exon 20 insertion mutations while sparing wild-type (WT) EGFR. IC50 values ranges from 1.1 ± 0.1 to 8.0 ± 1.1 nmol/L.
S8817 Almonertinib (HS-10296) Almonertinib (Aumolertinib, HS-10296, Ameile) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.
Biochem Pharmacol, 2021, 188:114516
S8852 Pyrotinib (SHR-1258) dimaleate Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor of EGFR and HER2 with IC50 of 0.013 μM and 0.038 μM, respectively.
Transl Lung Cancer Res, 2021, 10(8):3659-3670
Biomed Chromatogr, 2021, e5221
Clin Transl Med, 2020, 10(8):e254
S8920 (Rac)-JBJ-04-125-02 (Rac)-JBJ-04-125-02 (JBJ-04-125-02 racemate) is a mutant-selective allosteric inhibitor of Epidermal growth factor receptor (EGFR) with potential anticancer activity.
S8921 BI-4020 BI-4020 is an orally active, non-covalent EGFR inhibitor with IC50 of 0.6 nM and 0.2 nM for EGFRdel19 T790M C797S as biomarker potency and anti-proliferation potency in BaF3 cells, respectively.
S9414 Cyasterone Cyasterone is the main phytoecdysteroid component found in Cyathula capitata. It is a natural EGFR inhibitor and maybe a promising anti-cancer agent.
S9711 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
S9786 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
A2000 Cetuximab (anti-EGFR) Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW:145.781 KD.
Cell, 2022, 185(9):1521-1538.e18
Am J Cancer Res, 2022, 12(3):1393-1408
Adv Sci (Weinh), 2021, e2103360
S8312 NSC228155 NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.
Free Radic Biol Med, 2022, S0891-5849(22)00053-3
Cell Death Dis, 2021, 12(2):173
Am J Transl Res, 2020, 12(5):2295-2304
S6530 EBE-A22 EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
A2018New Panitumumab (anti-EGFR) Panitumumab (anti-EGFR, ABX-EGF) is a recombinant, fully human IgG2 monoclonal antibody that binds to the epidermal growth factor receptor (EGFR).
E0368New DZD9008 DZD9008 is an oral, potent, irreversible, wild type-selective EGFR inhibitor against EGFR or HER2 Exon20ins and other mutations with IC50 ranging from 0.4 nM to 2.1 nM for mutant EGFR.
E0822New AST-1306 AST-1306 (Allitinib) is an orally active and irreversible EGFR, ErbB2 and inhibitor with IC50s of 0.5, 3 and 0.8 nM, respectively.
E0833New O-Demethyl-Gefitinib O-Desmethyl gefitinib, a major active metabolite of gefitinib, is a potent EGFR (ErbB1/HER1) inhibitor, inhibits subcellular EGFR tyrosine kinase through a mechanism similar to that of gefitinib with IC50 values of 36 and 22 nM, respectively. 
S0070 Gefitinib-based PROTAC 3 Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
S0151 AG-1557 AG-1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
S0360 EGFR Inhibitor EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.
S0711 Canertinib dihydrochloride Canertinib (CI-1033, PD-183805, compound 18) dihydrochloride is a potent and irreversible inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Canertinib dihydrochloride inhibits cellular EGFR and ErbB2 autophosphorylation with IC50 of 7.4 nM and 9 nM, respectively.
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
Sci Rep, 2017,
BMC Cancer, 2017,
S0736 AG 556 AG 556 is an inhibitor of EGFR kinase autophosphorylation over HER1/2 autophosphorylation.
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Cell Death Dis, 2022, 13(6):524
Front Pharmacol, 2022, 13:807440
Int J Mol Med, 2022, 49(6)84
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Nature, 2022, 603(7900):335-342
Cancer Cell, 2022, S1535-6108(21)00662-0
Nat Immunol, 2022, 23(2):251-261
S1019 Canertinib (CI-1033) Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Acta Physiol (Oxf), 2021, 10.1111/apha.13661
S1023 Erlotinib (OSI-774) HCl Erlotinib (OSI-774, CP358774, NSC 718781) HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Sci Adv, 2022, 8(4):eabi7711
Neuro Oncol, 2022, noac105
J Cachexia Sarcopenia Muscle, 2022, 10.1002/jcsm.12985
S1025 Gefitinib (ZD1839) Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Mol Cancer, 2022, 21(1):43
Sci Adv, 2022, 8(4):eabi7711
Cell Rep, 2022, 39(4):110721
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x
Breast Cancer Res, 2022, 24(1):18
Mol Cancer Ther, 2022, molcanther.0320.2021
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Cancer Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
S1054 AG99 AG99 (Tyrphostin 46,Tyrphostin A46,Tyrphostin B40) is a potent and selective inhibitor of EGFR.
S1056 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
Genome Med, 2020, 18;12(1):17
PLoS Genet, 2016, 12(9):e1006279
Asian J Androl, 2016, 10.4103/1008-682X
S1079 PD153035 HCl PD153035 HCl (SU-5271 HCl, AG1517 HCl, ZM 252868 HCl) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
Int J Mol Sci, 2021, 22(8)3945
FEBS Lett, 2021, 595(5):563-576
FEBS Lett, 2021, 10.1002/1873-3468.14032
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
J Exp Med, 2022, 219(4)e20211498
J Headache Pain, 2022, 23(1):25
Mol Neurobiol, 2022, 59(5):3280-3293
S1167 CP-724714 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
Biochem J, 2021, BCJ20210173
Int J Mol Sci, 2020, 22(1)E82
NPJ Breast Cancer, 2020, 6:30
S1170 WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
Aging (Albany NY), 2020, 12(19):19022-19044
S1173 WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).
Cancers (Basel), 2021, 13(16)4133
Nat Nanotechnol, 2021, 10.1038/s41565-021-00872-w
Cell Res, 2020, 10.1038/s41422-020-00409-1
S1179 WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
Biochemistry, 2018, 57(8):1369-1379
Nat Commun, 2016, 7:10690
S1194 CUDC-101 CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.
Cancer Sci, 2020, 112(1):133-143
Anticancer Drugs, 2020, 31(2):158-168
NPJ Breast Cancer, 2020, 6:30
S1342 Genistein (NPI 031L) Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
S1486 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.
Cell Rep Med, 2022, 3(1):100492
Genome Med, 2020, 18;12(1):17
Mol Pharmacol, 2019, 95(5):528-536
S2111 Lapatinib (GW-572016) Lapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
Cancer Discov, 2022, 12(1):204-219
Cell Metab, 2022, 34(1):90-105.e7
Nat Chem Biol, 2022, 10.1038/s41589-022-00984-x