EGFR/ErbB1 Selective Inhibitors | Activators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S8312 NSC228155

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

Selective
S6546 PD153035

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

Selective EGFR, Ki: 5.2 pM
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.

Selective EGFR, Ki: 5.2 pM
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.

Selective EGFR (exon 19Del), IC50: 0.2 nM; EGFR (L858R), IC50: 0.2 nM; EGFR (WT), IC50: 0.3 nM
S7557 CL-387785 (EKI-785)

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

Selective EGFR, IC50: 370 pM
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.

Selective EGFR, IC50: 0.70 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).

Selective EGFR (L858R/T790M), IC50: 5 nM; EGFR (E746_A750/T790M), IC50: 14 nM; EGFR (E746_A750), IC50: 2 nM; EGFR (L858R), IC50: 2 nM
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.

Selective HER1/EGFR, IC50: 2 nM
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).

Selective EGFR (L858R/T790M), IC50: 8 nM; EGFR (L858R), IC50: 2 nM
S2205 OSI-420

OSI-420 (DesMethyl Erlotinib, CP-473420) is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

Selective EGFR, IC50: 2 nM
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.

Selective EGFR, IC50: 2 nM
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).

Selective EGFR, IC50: 3 nM
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.

Selective EGFR, IC50: 66 nM; EGFR (L858R), IC50: 5 nM; EGFR (L861Q), IC50: 4 nM
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.

Selective EGFR, IC50: 4 nM
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).

Selective EGFR, IC50: 5 nM
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.

Selective WT EGFR, IC50: 493.8 nM; L858R/T790M EGFR, IC50: 11.44 nM; Exon 19 deletion EGFR, IC50: 12.92 nM
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.

Selective EGFR, DC50: 22.3 nM; EGFR, DC50: 11.7 nM
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.

Selective EGFR, IC50: 15.5 nM
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.

Selective EGFR, IC50: 21 nM
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.

Selective EGFR (wt), Ki: 303.3 nM; EGFR (L858R/T790M), Ki: 21.5 nM
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.

Selective Tyr1173 (NR6W cells), IC50: 26 nM; Tyr992 (NR6W cells), IC50: 57 nM; Tyr992 (NR6wtEGFR cells), IC50: 37 nM; Tyr1173 (NR6wtEGFR cells), IC50: 37 nM
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.

Selective EGFR, IC50: 29 nM
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.

Selective EGFR, IC50: 38.5 nM
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.

Selective EGFR, IC50: 0.1 μM
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).

Selective EGFR, IC50: 500 nM
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.

Selective EGFR, IC50: 0.7 μM
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).

Selective EGFR, IC50: 1.2 μM
S2115 RG 13022

RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.

Selective EGFR, IC50: 4 μM
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.

Selective EGFR, IC50: 7.67 μM
S8009 AG-18

AG-18 (RG-50810, Tyrphostin A23, TX 825) inhibits EGFR with IC50 of 35 μM.

Selective EGFR, IC50: 35 μM
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.

Selective EGFR, IC50: 36.7 μM
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.

Selective EGFR, IC50: 460 μM
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.

Selective
S1179 WZ8040

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

Selective
S6523 RG14620

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

Selective
S1054 AG99

AG99 (Tyrphostin 46,Tyrphostin A46,Tyrphostin B40) is a potent and selective inhibitor of EGFR.

Selective
S6541 MTX-211

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

Selective
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.

Selective
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.

Selective
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.

Selective
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.

Selective
S2406 Chrysophanic Acid

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

Selective
S9711 CH7233163

CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.

Selective
S0151 AG-1557

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

Selective
S3759 Norcantharidin

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

Selective
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.

Selective
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.

Selective
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.

Selective
S8412 Naquotinib(ASP8273)

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

Pan
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.

Pan EGFR, Kd: 0.2 nM
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.

Pan EGFR (L858R/T790M), IC50: 10 nM; EGFR (wt), IC50: 0.5 nM; EGFR (L858R), IC50: 0.4 nM
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.

Pan EGFR (L858R/T790M), IC50: 10 nM; EGFR (L858R), IC50: 0.4 nM; EGFR (wt), IC50: 0.5 nM
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.

Pan EGFR (T790M/L858R), IC50: 12 nM; EGFR, IC50: 0.5 nM
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.

Pan EGFR (L861Q) , IC50: 1 nM; EGFR (wildtype), IC50: 25 nM; EGFR (L858R), IC50: 6 nM; EGFR (L858R/T790M), IC50: <1 nM
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.

Pan EGFR, IC50: 1.48 nM
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.

Pan EGFR, IC50: 1.5 nM
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.

Pan L858R/T790M EGFR, IC50: 2 nM; WT EGFR, IC50: 76 nM
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.

Pan EGFR, IC50: 2 nM
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.

Pan EGFR, IC50: 2.4 nM
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.

Pan WT EGFR, IC50: 3 nM
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.

Pan HER1, IC50: 3.2 nM
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.

Pan EGFR, IC50: 4 nM
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.

Pan EGFR WT, IC50: 8 nM; EGFR (T790M), IC50: 4.1 nM; EGFR (L861Q), IC50: 5.5 nM
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.

Pan EGFR, IC50: 6.0 nM
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.

Pan ErbB1, IC50: 7 nM
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.

Pan EGFR, IC50: 7.4 nM
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.

Pan EGFR, IC50: 10.8 nM
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.

Pan EGFR, IC50: 10.8 nM
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.

Pan EGFR, IC50: 0.013 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.

Pan mutant EGFR, IC50: <20 nM
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.

Pan HER1, IC50: 20 nM
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.

Pan EGFR/HER1, IC50: 23 nM
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.

Pan mutant EGFR, Ki: 0.031 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.

Pan EGFR, IC50: 92 nM
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.

Pan EGFR, IC50: 4.9 μM
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.

Pan
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.

Pan
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.

Pan