|
T9905 |
Cetuximab
|
Cetuximab (anti-EGFR),C225 |
EGFR
|
|
Cetuximab (C225) is a monoclonal antibody that is an inhibitor of human epidermal growth factor receptor (EGFR) (Kd=0.201 nM). Cetuximab has antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis. |
|
T5168 |
EGFR-IN-12
|
EGFR Inhibitor |
Apoptosis
,
EGFR
|
|
EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells. |
|
T9927 |
Panitumumab
|
|
EGFR
|
|
Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR). |
|
T76697 |
Panitumumab (anti-EGFR)
|
|
|
|
Panitumumab, a fully human IgG2 anti-EGFR monoclonal antibody, exerts anti-tumor effects by inhibiting tumor cell proliferation, survival, and angiogenesis. It is utilized in researching various cancers, including colon ... |
|
T9912 |
Trastuzumab
|
|
EGFR
|
|
Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastr... |
|
T8872 |
(Rac)-JBJ-04-125-02
|
JBJ-04-125-02 |
EGFR
|
|
(Rac)-JBJ-04-125-02 (JBJ-04-125-02) is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer. |
|
T7322 |
Theliatinib
|
|
EGFR
|
|
Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively. |
|
T23127 |
PD-161570
|
PD 161570 |
EGFR
,
FGFR
,
PDGFR
,
Src
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, a... |
|
T14336 |
Allitinib
|
AST-1306,ALS 1306 |
EGFR
|
|
Allitinib (AST-1306) (AST-1306) has anti-cancer activity，and it is an irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. [1] |
|
T9922 |
Matuzumab
|
|
EGFR
|
|
Matuzumab is a humanized monoclonal antibody used in cancer treatment. It has a high affinity for EGFR frequently associated with the growth of blood vessels in malignancy facilitating tumor growth and survival. |
|
T6331 |
Allitinib tosylate
|
AST-1306 TsOH,AST-6,Allitinib,AST-1306,AST-1306 (TsOH) |
EGFR
,
FLT
|
|
Allitinib tosylate (AST-1306) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively. |
|
T77746 |
Tyrosine kinase-IN-7
|
|
EGFR
,
Antiviral
|
|
Tyrosine kinase-IN-7 is a potent inhibitor of the tyrosine kinase EGFR, inhibiting EGFR(WT) and EGFR(T790M) and showing anti-cancer and anti-tumor activity in a variety of cancer cell lines. Tyrosine kinase-IN-7 has pote... |
|
T16343 |
NRC-2694
|
|
EGFR
|
|
NRC-2694 is an antagonist of the epidermal growth factor receptor (EGFR). It has anti-cancer and anti-proliferative properties. |
|
T61486 |
DHFR-IN-4
|
|
DHFR
|
|
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with anti-tumour activity, inhibits EGFR and HER2 and can be used to study pancreatic cancer. |
|
T76796 |
Patritumab
|
U3-1287,AMG-888 |
ERK
,
EGFR
,
Akt
,
HER
|
|
Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-sm... |
|
T12777 |
RTC-5
|
TRC-382 |
EGFR
|
|
RTC-5 (TRC-382) is a phenothiazine compound that has been specifically enhanced for its potent anti-cancer properties. It exhibits considerable effectiveness against an EGFR-driven cancer xenograft model. The mechanism ... |
|
T4346 |
SPDB
|
|
Others
|
|
SPDB is a small fragment linked to DM4 conjugates. It conjugates to antibodies utilizing disulfide linkers: anti-EGFR-SPDB-DM4 has been widely used. |
|
T35528L |
TD52 dihydrochloride
|
TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl |
Others
|
|
TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signali... |
|
TQ0271 |
Falnidamol
|
BIBX 1382 |
EGFR
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine k... |
|
T76833 |
Tomuzotuximab
|
|
|
|
Tomuzotuximab, a fully human glycoengineered IgG1 monoclonal antibody targeting EGFR (Anti-Human EGFR Recombinant Antibody), exhibits anticancer effects [1]. |
|
T30849 |
CGP-59326
|
UNII-YP9UZR062O,CGP59326,CGP 59326,TRX-13 |
|
|
CGP-59326 is an epidermal growth factor receptor (EGFR) antagonist, which is used in anti-cancer research. |
|
T72788 |
EGFR/C797S-IN-1
|
|
|
|
EGFR/C797S-IN-1 is a potent inhibitor targeting the EGFR-C797S mutation, demonstrated by its IC 50 value of 0.128 µM. This compound exhibits significant anti-proliferative and anti-tumor effects by inhibiting p-EGFR expr... |
|
T73154 |
EGFR-IN-70
|
|
|
|
EGFR-IN-70 is a potent EGFR inhibitor with IC 50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT , respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR . EGFR-IN-... |
|
T63648 |
EGFR kinase inhibitor 1
|
|
|
|
EGFR kinase inhibitor 1 is a potent inhibitor of EGFR that acts on WT (IC50: 37 nM), l885R/T790M (IC50: 1.7 nM), and L858R/T790M/C797S (IC50>300 nM). EGFR kinase inhibitor 1 is capable of blocking the cell cycle in G0/G1... |
|
T63161 |
EGFR/HER2/CDK9-IN-3
|
|
|
|
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM). EGFR/HER2/CDK9-IN-3 showed significant anti-tumor effects. |
|
T62746 |
EGFR/HER2/CDK9-IN-1
|
|
|
|
EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent EGFR/HER2/CDK9 inhibitor with IC50 values of 90.17, 131.39 and 67.04 nM. EGFR/HER2/CDK9-IN-1 exhibits significant anti-tumour effects. |
|
T63996 |
EGFR-IN-50
|
|
|
|
EGFR-IN-50 is a potent EGFR inhibitor targeting L858R resistance mutations, acting on TEL-EGFR-L858R-BaF3 and TEL-EGFR-T790M-L858R-BaF3 with GI50 values of 8 nM and 6.03 μM, respectively. EGFR-IN-50 exhibits anti-prolife... |
|
T81773 |
Modotuximab
|
Sym 004,DS 1024 |
|
|
Modotuximab (Anti-Human EGFR Recombinant Antibody), an IgG1κ-type chimeric antibody, selectively binds to human EGFR protein. Incorporating elements from Futuximab, it targets two distinct, non-overlapping epitopes on EG... |
|
T77050 |
Laprituximab
|
|
|
|
Laprituximab (J2898A), a humanized IgG1 anti-EGFR antibody, is utilized in the synthesis of the antibody-drug conjugate (ADC) IMGN289 [1]. |
|
T82193 |
HJM-561
|
|
PROTACs
|
|
HJM-561 is a potent and selective EGFR PROTAC with oral bioavailability, capable of overcoming osimertinib-resistant EGFR triple mutations and demonstrating anti-tumor activity [1]. |
|
T74457 |
EGFR-IN-42
|
|
|
|
EGFR-IN-42 (Compound 17b), a potent EGFR inhibitor, demonstrates single-digit nanomolar activity by covalently linking tamoxifen or endoxifen with gefitinib, retaining both ER antagonist activity and EGFR inhibition, res... |
|
T77073 |
Losatuxizumab
|
|
|
|
Losatuxizumab (ABT-806), an anti-EGFR monoclonal antibody, exhibits selective binding affinity towards various EGFR forms, with EC50 values of 0.96 nM for the wild-type EGFR, 0.09 nM for the C271A,C283A mutant, 0.12 nM f... |
|
T64253 |
EGFR/HER2-IN-4
|
|
|
|
EGFR/HER2-IN-4 is an irreversible, orally active dual inhibitor of EGFR activity (IC50: 0.6 nM). EGFR/HER2-IN-4 shows potent EGFR kinase inhibitory activity against L858R and T790M mutations. EGFR/HER2-IN-4 exhibits sign... |
|
T64254 |
EGFR/HER2-IN-5
|
|
|
|
EGFR/HER2-IN-5 is an irreversible, orally active dual inhibitor of EGFR activity (IC50: 0.6 nM). EGFR/HER2-IN-4 shows potent EGFR kinase inhibitory activity against L858R and T790M mutations. EGFR/HER2-IN-4 exhibits sign... |
|
T74458 |
EGFR-IN-43
|
|
|
|
EGFR-IN-43 (Compound 17c) is a highly effective EGFR inhibitor, exhibiting activity in the single-digit nanomolar range. It uniquely combines tamoxifen or endoxifen with the EGFR inhibitor gefitinib through a covalent bo... |
|
T78940 |
EGFR-IN-78
|
|
Apoptosis
|
|
EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer. It exhibits anti-proliferative properties, impedes EGFR phosphorylation, and induces G2/M... |
|
T70227 |
BPIQ-I
|
PD 159121 |
|
|
BPIQ-I (PD 159121), an ATP-competitive EGFR tyrosine kinase inhibitor, exhibits potent anti-proliferative activity. |
|
T79394 |
ALK/EGFR-IN-3
|
|
|
|
ALK/EGFR-IN-3 is a dual ALK and EGFR inhibitor that demonstrates potent anti-proliferative effects on various cancer cell lines, including H1975, PC9, and Baf3-EML4-ALK, with respective IC50 values of 0.1360, 0.0332, and... |
|
T74367 |
SC209
|
|
|
|
SC209, an ADC cytotoxin is used in synthesis of anti- EGFR antibody-drug conjugate ADC. SC209 is a metabolite of STRO-002 [1] [2] . |
|
T61077 |
UNC-CA359
|
|
|
|
UNC-CA359 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 18 nM. With strong anti-tumor activity, UNC-CA359 holds significant potential for chordoma research [1... |
|
T62503 |
EGFR/BRAFV600E-IN-1
|
|
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent dual inhibitor of EGFR (IC50: 0.08 μM) and BRAFV600E (IC50: 0.15 μM). EGFR/BRAFV600E-IN-1 exhibited anti-proliferative effects on A-549 (IC50: 1.2 μM), MCF-7 (IC50: 0.79 μM),... |
|
T82582 |
Depatuxizumab MMAE
|
|
|
|
Depatuxizumab MMAE is an antibody-drug conjugate (ADC) composed of the anti-EGFR monoclonal antibody depatuxizumab linked to the cytotoxic agent monomethyl auristatin E (MMAE). This ADC effectively suppresses the growth ... |
|
T78326 |
Depatuxizumab
|
ABT-806 |
EGFR
|
|
Depatuxizumab, a brain-penetrant, humanized anti-EGFR monoclonal antibody, selectively inhibits the growth of mutant EGFRvIII and wild-type EGFR xenograft models, and is utilized for research on cancer [1]. |
|
T76812 |
Intetumumab
|
|
|
|
Intetumumab (CNTO 95), a glycoengineered anti-EGFR monoclonal antibody designed for improved antibody-dependent cellular cytotoxicity (ADCC), is utilized in cancer research [1] [2]. |
|
T72818 |
Dosimertinib-d
|
|
|
|
Dosimertinib-d3-d3 is a potent, orally active inhibitor of EGFR, known to reduce the expression of p-EGFR and p-ERK proteins, thereby exhibiting antiproliferative and anti-tumor effects. It holds promise for research int... |
|
T78788 |
EGFR-IN-82
|
|
EGFR
|
|
EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R/T790M/C797S and 0.06 nM for EGFR Del19/T790M/C797S. It lacks significant inhibitory effects on EGFR ... |
|
T11714 |
JBJ-04-125-02
|
|
JAK
|
|
JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor w... |
|
T79729 |
EGFR/CDK2-IN-4
|
|
EGFR
|
|
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor targeting EGFR and CDK-2, demonstrating IC50 values of 89.6 nM for EGFR and 165.4 nM for CDK-2. It prompts apoptosis in MCF-7 cells and causes S phase cell cycle arrest, e... |
|
T35916 |
Simotinib
|
AL-6802,SIM-6802 |
EGFR
|
|
Simotinib (AL-6802) is a selective and orally bioactive EGFR tyrosine kinase inhibitor (IC50: 19.9 nM) with anti-tumour activity for the study of non-small cell lung cancer. |
|
T79728 |
EGFR/CDK2-IN-3
|
|
EGFR
|
|
EGFR/CDK2-IN-3 (compound 4b) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 71.7 nM and 113.7 nM, respectively. It prompts apoptosis in MCF-7 cells and halts the cell cycle in the S p... |
