• 阻害剤の選択性比較
  • 溶解度
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
S2150 Neratinib (HKI-272) <1 mg/mL 5 mg/mL <1 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
S2752 HER2-Inhibitor-1 <1 mg/mL 100 mg/mL 3 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 (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
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
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 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
S7298 AZ5104 <1 mg/mL 97 mg/mL 23 mg/mL
S7297 AZD9291 <1 mg/mL 99 mg/mL 43 mg/mL
S7557 CL-387785 (EKI-785) <1 mg/mL 63 mg/mL <1 mg/mL
S8294 Olmutinib (HM61713, BI 1482694) <1 mg/mL 97 mg/mL 23 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 91 mg/mL 20 mg/mL
S7358 Poziotinib (HM781-36B) <1 mg/mL 98 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, NVS-816) <1 mg/mL 99 mg/mL 99 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
S8312 NSC228155 <1 mg/mL 15 mg/mL <1 mg/mL


製品コード 製品説明 文献中の使用例 お客様のフィードバック

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.


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.


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.


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.


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.



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


Lifirafenib (BGB-283)

Lifirafenib (BGB-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.



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.



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.


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.



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.


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.



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.


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.



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).


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.



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.


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.


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.


Pelitinib (EKB-569)

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


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.


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.


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.



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



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).



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



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.


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.



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.



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



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).



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.



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.



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.



PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.


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.



CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.



AG-18 inhibits EGFR with IC50 of 35 μM.



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.



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.


CL-387785 (EKI-785)

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


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.


(-)-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.



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


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.



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.


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.



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


Chrysophanic Acid

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


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.


Lidocaine hydrochloride

Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.



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.



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



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