EGFR
EGFR (epidermal growth factor receptor) is the cell-surface receptor of its specific ligands, including epidermal growth factor and TGFα (transforming growth factor α) and is a receptor tyrosine kinase.
Products for EGFR
- Cat.No. Product Name Information
- GC38006 β-Hydroxyisovalerylshikonin Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
- GC63797 (S)-Sunvozertinib (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
- GC13257 AC480 (BMS-599626) AC480 (BMS-599626) (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. AC480 (BMS-599626) displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. AC480 (BMS-599626) inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
- GC11892 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
- GC11744 AG 555 Potent EGFR-kinase inhibitor
- GC13168 AG 825 Selective ErbB2 inhibitor
- GC14494 AG 99 AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
- GC17226 AG-1478 EGFR inhibitor,potent and selective
- GC12864 AG-1557 inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase
- GC17647 AG-18 AG-18 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
- GC13854 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) (Tyrphostin AG-490 (Tyrphostin B42)) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
- GC64398 Almonertinib mesylate Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
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GC67749
Amivantamab
Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity
- GC17283 AP26113 AP26113 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
- GC12478 ARRY-380 ARRY-380, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.
- GC11691 AST-1306 AST-1306 (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 is an anilino-quinazoline compound and has anti-cancer activity.
- GC15669 AST-1306 TsOH AST-1306 TsOH (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 TsOH also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 TsOH is an anilino-quinazoline compound and has anti-cancer activity
- GC33096 AST2818 mesylate Alflutinib (Furmonertinib) mesylate is is a potent inhibitor of EGFR. Alflutinib (Furmonertinib) mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Alflutinib (Furmonertinib) mesylate has the potential for the research of cancer diseases, especially non-small cell lung cancer (NSCLC).
- GC35413 Astragaloside VI Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
- GC35435 AV-412 A dual inhibitor of EGFR and HER2
- GC35436 AV-412 free base AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
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GC19044
Avitinib maleate
A pyrrolopyrimidine-based irreversible EGFR inhibitor
- GC12955 AZ5104 EGFR inhibitor
- GC16308 AZD-9291 AZD-9291 (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. AZD-9291 overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
- GC16698 AZD-9291 mesylate AZD-9291 mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
- GC13143 AZD3759 AZD3759 (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively.
- GC13761 AZD8931 (Sapitinib) AZD8931 (Sapitinib) (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
- GC64302 BAY 2476568 BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG).
- GC64017 Befotertinib Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
- GC33172 BGB-102 (JNJ-26483327) BGB-102 (JNJ-26483327) is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
- GC19066 BGB-283 BGB-283 is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
- GC38402 BI-4020 A fourth-generation and non-covalent EGFR tyrosine kinase inhibitor
- GC63910 BLU-945 BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).
- GC10944 Butein Protein kinase inhibitor
- GC12910 Canertinib (CI-1033) Canertinib (CI-1033) (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
- GC34217 Cetuximab (C225) Cetuximab (C225) (C225) is a human IgG1 monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab (C225) has potent antitumor activity.
- GC15950 CGP 52411 EGFR inhibitor
- GC25219 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
- GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
- GC17790 CL-387785 (EKI-785) CL-387785 (EKI-785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.
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GC11264
CNX-2006
mutant-EGFR inhibitor, selective and irreversible
- GC13091 CP-724714 HER2 inhibitor,potent and selective
- GC38180 Cyasterone
- GC10225 Dacomitinib (PF299804, PF299) Dacomitinib (PF299804, PF299) (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
- GC64039 Disitamab vedotin Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent Monomethyl auristatin E (MMAE). Disitamab vedotin enhances antitumor immunity.
- GC66432 EAI001 EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.
- GC12281 EAI045 Inhibitor of L858R/T790M EGFR mutants
- GC16321 EGF816 EGF816 (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min-1 on EGFR(L858R/790M) mutant, respectively.
- GC35965 EGFR mutant-IN-1 EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
- GC65572 EGFR Protein Tyrosine Kinase Substrate EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.
- GC64497 EGFR-IN-17 EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
- GC33195 EGFR-IN-2 EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
- GC19132 EGFR-IN-3 EGFR-IN-3 is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. EGFR-IN-3 has the potential for NSCLC research.
- GC66428 EGFR-IN-5 EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
- GC68440 EGFR-IN-69
- GC35966 EGFR-IN-7 EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 shows anti-tumor activity. EGFR-IN-7 can be used for the research of various cancers.
- GC65974 EGFR-IN-9 EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
- GC33048 Epertinib (S-22611) Epertinib (S-22611) (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib (S-22611) shows potent antitumor activity.
- GC38350 Epertinib hydrochloride Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
- GC36003 Erlotinib mesylate EGFR inhibitor
- GC65992 FGFR2-IN-3 FGFR2-IN-3 is an orally active selective inhibitor of FGFR2.
- GC65991 FGFR2-IN-3 hydrochloride FGFR2-IN-3 hydrochloride is an orally active selective inhibitor of FGFR2.
- GC36044 FIIN-3 FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
- GC19509 Gefitinib-based PROTAC 3 A VHL-recruiting PROTAC
- GC14102 Genistein Genistein is an isoflavone belonging to the flavonoid group of compounds and is found in a number of plants.
- GC33053 HS-10296 hydrochloride Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. HS-10296 hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). HS-10296 hydrochloride is used for the research of the non-small cell lung cancer.
- GC17982 Icotinib EGFR tyrosine kinase inhibitor
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GC67690
JBJ-09-063 hydrochloride
JBJ-09-063 hydrochloride is a mutation selective allosteric EGFR inhibitor
- GC67860 JBJ-09-063 TFA
- GC65436 JND3229 JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
- GC25559 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.
- GC67759 Lapatinib-d4
- GC16021 Lavendustin A EGFR tyrosine kinase inhibitor
- GC19218 Lazertinib Lazertinib is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
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GC69410
Lumretuzumab
Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized monoclonal antibody that targets HER3 (ERBB3) and can be used for cancer research.
- GC68304 Margetuximab
- GC64710 MC-Val-Cit-PAB-Amide-TLR7 agonist 4 MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
- GC19256 MTX-211 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
- GC10250 Mubritinib (TAK 165) Mubritinib (TAK 165) (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
- GC11126 Mutant EGFR inhibitor Selective Mutated EGFR inhibitor
- GC36666 Mutated EGFR-IN-1 Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
- GC36667 Mutated EGFR-IN-2 Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
- GC33022 Naquotinib (ASP8273) Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
- GC32836 Naquotinib mesylate (ASP8273) Naquotinib mesylate (ASP8273) (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
- GC36699 Nazartinib mesylate Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
- GC10362 Neratinib (HKI-272) Neratinib (HKI-272) (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
- GC33131 NRC-2694 NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
- GC14103 NSC228155 EGFR activator
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GC69596
NSC689857
NSC689857 is an effective inhibitor of EGFR and SCFSKP2, with an IC50 of 36 μM against Skp2-Cks1. NSC689857 can inhibit phosphorylation of p27 (IC50=30 μM). NSC689857 exhibits varying activity in different types of cancer, with higher resistance activity against leukemia cell lines compared to other cancer cells.
- GC44491 O-Desmethyl Gefitinib O-Desmethyl gefitinib is the major metabolite of gefitinib in human plasma, formed by the cytochrome P450 isoform CYP2D6.
- GC68321 O-Desmethyl gefitinib-d8
- GC15370 Olmutinib (HM61713, BI 1482694) Olmutinib (HM61713, BI 1482694) (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib (HM61713, BI 1482694) is used for NSCLC.
- GC64770 Oritinib Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
- GC17530 OSI-420 OSI-420 (OSI-420) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.
- GC36819 Osimertinib dimesylate Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
- GC66405 Panitumumab Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer.
- GC66333 Panitumumab (anti-EGFR) Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer.
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GC69665
Patritumab
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody targeting ERBB3. Patritumab has synergistic effects with Cetuximab and can effectively inhibit the phosphorylation of EGFR, HER2, HER3, ERK and AKT. Patritumab also induces apoptosis and inhibits the growth of pancreatic, non-small cell lung cancer and colorectal cancer xenograft tumors.
- GC15925 PD 158780 ErbB receptor family tyrosine kinase inhibitor
- GC34105 PD153035 Hydrochloride (ZM 252868) A highly potent EGFR inhibitor