EGFR

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1023 Erlotinib HCl (OSI-744) <1 mg/mL 4 mg/mL <1 mg/mL
S1025 Gefitinib (ZD1839) <1 mg/mL 89 mg/mL 4 mg/mL
S1028 Lapatinib (GW-572016) Ditosylate <1 mg/mL 100 mg/mL <1 mg/mL
S1011 Afatinib (BIBW2992) <1 mg/mL 97 mg/mL 15 mg/mL
S2150 Neratinib (HKI-272) <1 mg/mL 5 mg/mL <1 mg/mL
S7824 Nazartinib (EGF816, NVS-816) <1 mg/mL 99 mg/mL 99 mg/mL
S8412 Naquotinib(ASP8273) <1 mg/mL 52 mg/mL 100 mg/mL
S8312 NSC228155 <1 mg/mL 58 mg/mL <1 mg/mL
S8294 Olmutinib (HM61713, BI 1482694) <1 mg/mL 97 mg/mL 23 mg/mL
S1019 Canertinib (CI-1033) <1 mg/mL 2 mg/mL 9 mg/mL
S2111 Lapatinib <1 mg/mL 100 mg/mL <1 mg/mL
S1143 AG-490 (Tyrphostin B42) <1 mg/mL 59 mg/mL 6 mg/mL
S1167 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
S2727 Dacomitinib (PF299804, PF299) <1 mg/mL 19 mg/mL <1 mg/mL
S1173 WZ4002 <1 mg/mL 13 mg/mL <1 mg/mL
S2192 Sapitinib (AZD8931) <1 mg/mL 40 mg/mL <1 mg/mL
S1194 CUDC-101 <1 mg/mL 20 mg/mL <1 mg/mL
S2728 AG-1478 (Tyrphostin AG-1478) <1 mg/mL 25 mg/mL 13 mg/mL
S1079 PD153035 HCl <1 mg/mL 0.5 mg/mL <1 mg/mL
S1392 Pelitinib (EKB-569) <1 mg/mL 13 mg/mL <1 mg/mL
S1056 AC480 (BMS-599626) <1 mg/mL 113 mg/mL 20 mg/mL
S1486 AEE788 (NVP-AEE788) <1 mg/mL 88 mg/mL <1 mg/mL
S2205 OSI-420 <1 mg/mL 83 mg/mL <1 mg/mL
S1170 WZ3146 <1 mg/mL 93 mg/mL <1 mg/mL
S1179 WZ8040 <1 mg/mL 96 mg/mL 3 mg/mL
S2185 AST-1306 <1 mg/mL 124 mg/mL <1 mg/mL
S7284 Rociletinib (CO-1686, AVL-301) <1 mg/mL 100 mg/mL <1 mg/mL
S1342 Genistein <1 mg/mL 54 mg/mL 2 mg/mL
S2755 Varlitinib <1 mg/mL 6 mg/mL <1 mg/mL
S2922 Icotinib <1 mg/mL 78 mg/mL 7 mg/mL
S2784 TAK-285 <1 mg/mL 110 mg/mL 54 mg/mL
S2867 WHI-P154 <1 mg/mL 75 mg/mL <1 mg/mL
S2554 Daphnetin <1 mg/mL 35 mg/mL <1 mg/mL
S7039 PD168393 <1 mg/mL 74 mg/mL <1 mg/mL
S2895 Tyrphostin 9 <1 mg/mL 56 mg/mL 56 mg/mL
S7206 CNX-2006 <1 mg/mL 100 mg/mL 29 mg/mL
S8009 AG-18 <1 mg/mL 37 mg/mL 37 mg/mL
S7298 AZ5104 <1 mg/mL 97 mg/mL 23 mg/mL
S7297 Osimertinib (AZD9291) <1 mg/mL 99 mg/mL 43 mg/mL
S7557 CL-387785 (EKI-785) <1 mg/mL 63 mg/mL <1 mg/mL
S2250 (-)-Epigallocatechin Gallate 23 mg/mL 72 mg/mL 83 mg/mL
S7786 Erlotinib <1 mg/mL 78 mg/mL 15 mg/mL
S7810 Afatinib (BIBW2992) Dimaleate <1 mg/mL 100 mg/mL <1 mg/mL
S7971 AZD3759 <1 mg/mL 92 mg/mL 44 mg/mL
S7358 Poziotinib (HM781-36B) <1 mg/mL 98 mg/mL <1 mg/mL
S2406 Chrysophanic Acid <1 mg/mL 5 mg/mL <1 mg/mL
S8036 Butein <1 mg/mL 55 mg/mL 55 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1023

Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744) 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.

S1025

Gefitinib (ZD1839)

Gefitinib (ZD-1839) 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.

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.

S1011

Afatinib (BIBW2992)

Afatinib (BIBW2992) 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 in cell-free assays, respectively.

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.

S7824New

Nazartinib (EGF816, NVS-816)

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.

S8412New

Naquotinib(ASP8273)

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

S8294New

Olmutinib (HM61713, BI 1482694)

Olmutinib 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.

S1019

Canertinib (CI-1033)

Canertinib (CI-1033) 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.

S2111

Lapatinib

Lapatinib, 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.

S1143

AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42) 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.

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.

S2727

Dacomitinib (PF299804, PF299)

Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.

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).

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.

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.

S2728

AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478) 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.

S1079

PD153035 HCl

PD153035 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.

S1392

Pelitinib (EKB-569)

Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Phase2.

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.

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.

S2205

OSI-420

OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

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).

S1179

WZ8040

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

S2185

AST-1306

AST-1306 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.

S7284

Rociletinib (CO-1686, AVL-301)

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.

S1342

Genistein

Genistein, 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.

S2755

Varlitinib

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

S2922

Icotinib

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).

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.

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.

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.

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.

S2895

Tyrphostin 9

Tyrphostin 9 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.

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.

S8009

AG-18

AG-18 inhibits EGFR with IC50 of 35 μM.

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.

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.

S7557

CL-387785 (EKI-785)

CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.

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.

S7786

Erlotinib

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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.

S7971

AZD3759

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.

S7358

Poziotinib (HM781-36B)

Poziotinib (HM781-36B) 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. Phase 2.

S2406

Chrysophanic Acid

Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.

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.

S8312New

NSC228155

NSC228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.

Catalog No. Information Product Use Citations Product Validations
S1023

Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744) 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.

S1025

Gefitinib (ZD1839)

Gefitinib (ZD-1839) 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.

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.

S1011

Afatinib (BIBW2992)

Afatinib (BIBW2992) 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 in cell-free assays, respectively.

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.

S7824New

Nazartinib (EGF816, NVS-816)

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.

S8412New

Naquotinib(ASP8273)

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

S8294New

Olmutinib (HM61713, BI 1482694)

Olmutinib 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.

S1019

Canertinib (CI-1033)

Canertinib (CI-1033) 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.

S2111

Lapatinib

Lapatinib, 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.

S1143

AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42) 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.

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.

S2727

Dacomitinib (PF299804, PF299)

Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.

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).

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.

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.

S2728

AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478) 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.

S1079

PD153035 HCl

PD153035 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.

S1392

Pelitinib (EKB-569)

Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Phase2.

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.

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.

S2205

OSI-420

OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

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).

S1179

WZ8040

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

S2185

AST-1306

AST-1306 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.

S7284

Rociletinib (CO-1686, AVL-301)

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.

S1342

Genistein

Genistein, 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.

S2755

Varlitinib

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

S2922

Icotinib

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).

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.

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.

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.

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.

S2895

Tyrphostin 9

Tyrphostin 9 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.

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.

S8009

AG-18

AG-18 inhibits EGFR with IC50 of 35 μM.

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.

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.

S7557

CL-387785 (EKI-785)

CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.

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.

S7786

Erlotinib

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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.

S7971

AZD3759

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.

S7358

Poziotinib (HM781-36B)

Poziotinib (HM781-36B) 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. Phase 2.

S2406

Chrysophanic Acid

Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.

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.

Catalog No. Information Product Use Citations Product Validations
S8312New

NSC228155

NSC228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.

Tags: EGFR inhibition | EGFR cancer | EGFR tumor | EGFR activation | EGFR signaling pathway | EGFR phosphorylation | EGFR targets | EGFR inhibitor drugs | EGFR inhibitors cancer | EGFR assay | EGFR activity | EGFR inhibitors list | EGFR inhibitor review