EGFR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
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
S1006 Saracatinib (AZD0530) <1 mg/mL 35 mg/mL 31 mg/mL
S6899 Licochalcone D -1 mg/mL 100 mg/mL -1 mg/mL
S6897 Epertinib hydrochloride <1 mg/mL 100 mg/mL <1 mg/mL
S8584 Theliatinib (HMPL-309) -1 mg/mL 47 mg/mL -1 mg/mL
S6868 Alflutinib (AST2818) mesylate <1 mg/mL 20 mg/mL <1 mg/mL
S8852 Pyrotinib (SHR-1258) <1 mg/mL <1 mg/mL <1 mg/mL
S6805 Tyrphostin AG-528 ˂1 mg/mL 61 mg/mL 5 mg/mL
S6813 Mobocertinib (TAK788) <1 mg/mL 9 mg/mL <1 mg/mL
S0360 EGFR Inhibitor ˂1 mg/mL 83 mg/mL 2 mg/mL
S0151 AG-1557 <1 mg/mL 40 mg/mL 3 mg/mL
S0070 Gefitinib-based PROTAC 3 <1 mg/mL 100 mg/mL 100 mg/mL
S6809 SU5214 <1 mg/mL 50 mg/mL <1 mg/mL
S2115 RG 13022 <1 mg/mL 53 mg/mL 5 mg/mL
S1054 AG99 <1 mg/mL 41 mg/mL <1 mg/mL
S6698 TQB3804 (EGFR-IN-7) <1 mg/mL <1 mg/mL <1 mg/mL
S1046 Vandetanib (ZD6474) <1 mg/mL 4 mg/mL <1 mg/mL
S2150 Neratinib (HKI-272) <1 mg/mL 5 mg/mL <1 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 58 mg/mL 6 mg/mL
S1167 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
S2727 Dacomitinib (PF-00299804) <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
S7000 AP26113-analog (ALK-IN-1) <1 mg/mL 45 mg/mL 106 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
S2752 HER2-Inhibitor-1 <1 mg/mL 100 mg/mL 3 mg/mL
S1179 WZ8040 <1 mg/mL 96 mg/mL 3 mg/mL
S2185 Allitinib (AST-1306) <1 mg/mL 124 mg/mL <1 mg/mL
S7284 Rociletinib (CO-1686) <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 73 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
S6525 AG 555 <1 mg/mL 64 mg/mL 64 mg/mL
S7298 AZ5104 <1 mg/mL 97 mg/mL 23 mg/mL
S8724 Lazertinib <1 mg/mL 4 mg/mL <1 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
S6509 AG 494 <1 mg/mL 56 mg/mL 4 mg/mL
S8362 Tucatinib (Irbinitinib, ONT-380) <1 mg/mL 96 mg/mL 15 mg/mL
S8294 Olmutinib (BI 1482694) <1 mg/mL 97 mg/mL 23 mg/mL
S6523 RG14620 <1 mg/mL 55 mg/mL 6 mg/mL
S6546 PD153035 <1 mg/mL 6 mg/mL <1 mg/mL
S6541 MTX-211 <1 mg/mL 24 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
S5098 Gefitinib hydrochloride 1 mg/mL 8 mg/mL 1 mg/mL
S7810 Afatinib (BIBW2992) Dimaleate <1 mg/mL 100 mg/mL <1 mg/mL
S7971 AZD3759 <1 mg/mL 91 mg/mL 20 mg/mL
S7358 Poziotinib (HM781-36B) <1 mg/mL 98 mg/mL <1 mg/mL
S8229 Brigatinib (AP26113) <1 mg/mL 1 mg/mL 43 mg/mL
S5078 Osimertinib mesylate -1 mg/mL 9 mg/mL -1 mg/mL
S8412 Naquotinib(ASP8273) <1 mg/mL 52 mg/mL 100 mg/mL
S2406 Chrysophanic Acid <1 mg/mL 5 mg/mL <1 mg/mL
S7824 Nazartinib (EGF816) <1 mg/mL 99 mg/mL 99 mg/mL
S3759 Norcantharidin -1 mg/mL 33 mg/mL -1 mg/mL
S7926 Lifirafenib (BGB-283) <1 mg/mL 95 mg/mL 95 mg/mL
S4667 Lidocaine hydrochloride 54 mg/mL 54 mg/mL 54 mg/mL
S8036 Butein <1 mg/mL 55 mg/mL 55 mg/mL
S8242 EAI045 <1 mg/mL 76 mg/mL <1 mg/mL
S8814 TAS6417 <1 mg/mL 79 mg/mL 79 mg/mL
S9414 Cyasterone -1 mg/mL 100 mg/mL -1 mg/mL
S8817 HS-10296 <1 mg/mL 100 mg/mL 6 mg/mL
S8741 Avitinib (AC0010) <1 mg/mL 97 mg/mL 97 mg/mL
S8312 NSC228155 <1 mg/mL 15 mg/mL <1 mg/mL
S6530 EBE-A22 <1 mg/mL 9 mg/mL <1 mg/mL

亜型選択性的な製品

EGFR製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

S1023

Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744, CP358774, NSC 718781) 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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

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) 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.

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.

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 activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

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.

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.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) 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.

S8852

Pyrotinib (SHR-1258)

Pyrotinib (SHR-1258, BLTN, Pyrroltinib) 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.

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.

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.

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.

S0151

AG-1557

AG-1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.

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.

S6809

SU5214

SU5214 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.

S2115

RG 13022

RG-13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.

S1054

AG99

AG99 is a potent and selective inhibitor of EGFR.

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.

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).

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.

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.

S2111

Lapatinib

Lapatinib (GSK572016), 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.

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.

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 (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.

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, 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).

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.

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.

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.

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.

S2205

OSI-420

OSI-420 (DesMethyl Erlotinib, CP-473420) 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).

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.

S1179

WZ8040

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

S2185

Allitinib (AST-1306)

Allitinib (AST-1306, 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.

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.

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 (ARRY334543) 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 (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).

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 (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.

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 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.

S6525

AG 555

AG-555 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.

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.

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.

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.

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).

S8362

Tucatinib (Irbinitinib, ONT-380)

Tucatinib (Irbinitinib, ONT-380, 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.

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.

S6523

RG14620

RG14620, an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2/BCRP.

S6546

PD153035

PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).

S6541

MTX-211

MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.

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 (CP358774, NSC 718781) 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.

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.

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.

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, 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.

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.

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.

S8412

Naquotinib(ASP8273)

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

S2406

Chrysophanic Acid

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

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.

S3759

Norcantharidin

Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

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.

S4667

Lidocaine hydrochloride

Lidocaine hydrochloride 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.

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.

S8242

EAI045

EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor.

S8814

TAS6417

TAS6417 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.

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.

S8817

HS-10296

HS-10296 (Almonertinib, Ameile) is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.

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.

S8312

NSC228155

NSC228155 is an activator of EGFR. It binds to the sEGFR dimerization domain II and modulates EGFR tyrosine phosphorylation.

S6530

EBE-A22

EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.

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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.

S1023

Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744, CP358774, NSC 718781) 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. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

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) 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.

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.

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 activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.

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.

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.

S6868

Alflutinib (AST2818) mesylate

Alflutinib (AST2818) 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.

S8852

Pyrotinib (SHR-1258)

Pyrotinib (SHR-1258, BLTN, Pyrroltinib) 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.

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.

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.

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.

S0151

AG-1557

AG-1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.

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.

S6809

SU5214

SU5214 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.

S2115

RG 13022

RG-13022 inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.

S1054

AG99

AG99 is a potent and selective inhibitor of EGFR.

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.

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).

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.

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.

S2111

Lapatinib

Lapatinib (GSK572016), 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.

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.

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 (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.

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, 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).

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.

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.

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.

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.

S2205

OSI-420

OSI-420 (DesMethyl Erlotinib, CP-473420) 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).

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.

S1179

WZ8040

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

S2185

Allitinib (AST-1306)

Allitinib (AST-1306, 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.

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.

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 (ARRY334543) 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 (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).

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 (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.

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 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.

S6525

AG 555

AG-555 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.

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.

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.

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.

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).

S8362

Tucatinib (Irbinitinib, ONT-380)

Tucatinib (Irbinitinib, ONT-380, 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.

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.

S6523

RG14620

RG14620, an EGFR inhibitor of the tyrphostin family, directly inhibits the transport function of ABCG2/BCRP.

S6546

PD153035

PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).

S6541

MTX-211

MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.

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 (CP358774, NSC 718781) 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.

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.

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.