Catalog No.
Product Name
Application
Product Information
Citations
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EGFR C797S Mutation Inhibitor
EGFR-IN-89 is a potent fourth-generation inhibitor targeting the EGFR C797S mutation, demonstrating an IC50 of 10.1 nM against Del19/T790M/C797S mutations. This compound exhibits enhanced selectivity over wild-type EGFR, making it a valuable tool for studying resistance mechanisms in non-small cell lung cancer (NSCLC) and other malignancies with EGFR mutations. Its application can significantly aid in the development of targeted therapies for patients with specific EGFR mutations. -
EGFR Inhibitor
Andamertinib is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting significant antineoplastic activity. This compound is primarily utilized in research related to targeted cancer therapies, particularly in the treatment of EGFR-mutant cancers. Its mechanism of action involves blocking EGFR signaling pathways, thereby inhibiting tumor growth and proliferation. -
EGFR
(3S,4S)-PF-06459988 is a selective irreversible inhibitor targeting the T790M mutant form of the epidermal growth factor receptor (EGFR). This compound demonstrates significant biological activity against mutant EGFR while exhibiting excellent selectivity for the wild-type receptor. Its design features a minimally reactive electrophile, which reduces the likelihood of off-target labeling, making it a valuable reagent for cancer research and studies investigating EGFR-driven pathways. -
EGFR Inhibitor
Methyl 2,5-dihydroxycinnamate is a potent inhibitor of epidermal growth factor receptor (EGFR) kinase activity, functioning as an erbstatin analog. This compound effectively disrupts EGFR signaling, making it a valuable tool in cancer research, particularly for studies focused on tumor growth and metastasis. Its stability and efficacy position it as an important reagent for elucidating the role of EGFR in various biological processes. -
EGFR Inhibitor
BEBT-109 is a potent pan-mutant-selective inhibitor of the epidermal growth factor receptor (EGFR). This compound exhibits enhanced pharmacokinetic properties, making it suitable for in-depth studies. BEBT-109 is primarily utilized in research focused on non-small cell lung cancer (NSCLC) driven by various EGFR mutations, enabling exploration of therapeutic strategies targeting this pathway. -
EGFR L858R/T790M Mutant Inhibitor
EGFR-IN-1 hydrochloride is an orally active and irreversible inhibitor targeting the mutant EGFR L858R/T790M. This compound exhibits potent inhibition of Gefitinib-resistant EGFR variants with a selectivity ratio of 100-fold over wild-type EGFR. Notably, EGFR-IN-1 hydrochloride demonstrates significant antiproliferative activity against H1975 and HCC827 cell lines, making it a valuable tool for antitumor research applications in cancer studies related to resistant EGFR mutations. -
EGFR Triple Mutant Inhibitor
EMI56 is a potent inhibitor of the EGFR triple mutant, demonstrating enhanced activity compared to its precursor, EMI1. This compound effectively targets and inhibits mutant forms of the epidermal growth factor receptor, making it valuable for research into EGFR-related pathologies, particularly in cancer models. EMI56 is suitable for studies focused on understanding resistance mechanisms and developing targeted therapeutic strategies. -
Dual EGFR/HER2 Inhibitor
Enozertinib is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), designed for oral administration with the ability to penetrate the central nervous system. This highly selective and irreversible compound effectively targets exon 20 insertion mutations, demonstrating significant antitumor activity and inducing tumor regression in models of central nervous system and non-small cell lung cancer (NSCLC). Enozertinib is valuable for research involving solid tumors and NSCLC, offering enhanced kinome selectivity to minimize off-target effects. -
EGFR L858R/T790M Mutant Inhibitor
EGFR-IN-1 is an orally active, irreversible inhibitor selectively targeting the EGFR L858R/T790M mutants. This compound demonstrates potent inhibition of Gefitinib-resistant EGFR variants with over 100-fold selectivity compared to wild-type EGFR. EGFR-IN-1 exhibits significant antiproliferative effects in both H1975 and mutated HCC827 cancer cell lines, indicating its potential utility in anticancer research and therapeutic applications. -
PROTAC EGFR Degrader
MS9427 is a selective PROTAC degrader targeting the epidermal growth factor receptor (EGFR), demonstrating Kd values of 7.1 nM and 4.3 nM for EGFR wild-type and L858R mutant forms, respectively. This compound effectively induces degradation of the mutant EGFR via both the ubiquitin/proteasome system and autophagy/lysosomal pathways, while sparing the wild-type receptor. MS9427 is a valuable tool for studying the proliferation inhibition of non-small cell lung cancer (NSCLC) cells and advancing anticancer research. -
EGFR Inhibitor
JBJ-09-063 is a mutant-selective allosteric inhibitor targeting the epidermal growth factor receptor (EGFR). It exhibits potent inhibitory activity with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. JBJ-09-063 effectively attenuates phosphorylation of EGFR, Akt, and ERK1/2, demonstrating its utility in both TKI-sensitive and resistant models. This compound is particularly valuable for studying EGFR-mutant lung cancer and exploring therapeutic strategies for treatment-resistant variants. -
EGFR Mutant Inhibitor
Mutated EGFR-IN-3 is a highly selective allosteric inhibitor targeting the mutant forms of epidermal growth factor receptor (EGFR), specifically EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S). It demonstrates potent ATP-competitive inhibition with IC50 values of 12 nM and 13 nM, respectively. This compound is valuable for research applications focused on understanding and treating cancers driven by these specific EGFR mutations. -
EGFR-TKI
Epitinib succinate is a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) that demonstrates effective oral bioavailability and optimized penetration into the central nervous system. This compound is primarily utilized in cancer research, offering insights into targeted therapies for EGFR-associated tumors. Additionally, Epitinib succinate features an alkyne moiety that enables its use in click chemistry, specifically in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating advanced biochemical studies. -
EGFR Inhibitor
EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 0.0002 μM. It is specifically designed to address C797S-mediated resistance, making it a valuable tool for researchers investigating EGFR-related pathways in cancer. This compound is applicable for studies focusing on therapeutic strategies against resistant forms of malignancies driven by EGFR signaling. -
HER2/EGFR Inhibitor
GW2974 is a potent dual inhibitor of the human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50 values of 0.007 μM and 0.016 μM, respectively. It effectively inhibits the proliferation of tumor cells in vitro, making it a valuable tool in cancer research. GW2974 is particularly relevant for studies focused on glioblastoma multiforme (GBM) and related malignancies. -
EGFR Ligand
EGFR ligand-9 is a specific ligand for the epidermal growth factor receptor (EGFR). It is designed for use in the synthesis of PROTAC EGFR degrader 9, facilitating the targeted degradation of EGFR in research applications. This compound is valuable for studying EGFR signaling pathways and developing novel therapeutic strategies in cancer research. -
EGFR/ErbB2 Inhibitor
Tephrosin is a natural rotenoid that functions as an inhibitor of the epidermal growth factor receptor (EGFR) and ErbB2. It demonstrates significant antitumor activity by promoting the internalization and subsequent degradation of these receptors, thereby disrupting downstream signaling pathways involved in cellular proliferation and survival. This compound is useful in cancer research, particularly in studies focusing on targeted therapies for EGFR and ErbB2-overexpressing tumors. -
EGFR/AURKB Inhibitor
EGFR/AURKB-IN-1 is a dual inhibitor targeting Epidermal Growth Factor Receptor (EGFR) and Aurora Kinase B (AURKB), effectively blocking their phosphorylation with IC50 values of 0.07 µM and 1.1 µM, respectively. This compound binds to the hydrophobic region I and αC-helix out pocket of EGFR, as well as the back pocket of AURKB, thereby inhibiting tumor cell growth, division, and metastasis. EGFR/AURKB-IN-1 is suitable for comprehensive cancer research applications aimed at elucidating mechanisms of tumor progression and therapy resistance. -
EGFR Inhibitor
PF-6274484 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), with inhibitory constants (Kis) of 0.14 nM for the EGFR-L858R/T790M mutant and 0.18 nM for wild-type EGFR. This compound effectively inhibits autophosphorylation of EGFR-L858R/T790M in H1975 cells and wild-type EGFR in A549 cells, demonstrating IC50 values of 6.6 nM and 5.8 nM, respectively. PF-6274484 is valuable for researching targeted therapies in EGFR-driven cancers and elucidating signaling pathways linked to tumor proliferation. -
EGFR/c-Met Inhibitor
EGFR-IN-8 is a dual inhibitor of the epidermal growth factor receptor (EGFR) and c-Met, demonstrating potential efficacy against EGFR TKI-resistant non-small cell lung cancer (NSCLC). This compound offers a novel approach for effectively targeting resistance mechanisms in NSCLC, providing a valuable tool for oncological research and drug development. Its unique pharmacological profile positions it as a promising candidate for further investigation in cancer therapy. -
EGFR Inhibitor
Dosimertinib-d5 mesylate is a potent, orally active inhibitor of the epidermal growth factor receptor (EGFR). It effectively reduces the levels of phosphorylated EGFR and ERK proteins, demonstrating significant antiproliferative and anti-tumor activities. This compound is particularly relevant for research applications focused on non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EAI001 is a potent allosteric inhibitor of the mutant epidermal growth factor receptor (EGFR), specifically targeting the EGFRL858R/T790M variant with an IC50 of 24 nM. This compound demonstrates selective inhibition of aberrant EGFR signaling, making it valuable for investigating its role in cancer biology and therapeutic resistance. EAI001 serves as a critical tool for research aimed at understanding and developing treatments for EGFR-mutated tumors. -
EGFR/ErbB Inhibitor
EGFR/ErbB-2-IN-2 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and ErbB family of receptor tyrosine kinases. It exhibits IC50 values of 0.017 μM for EGFR, 0.08 μM for ErbB-2, and 1.91 μM for ErbB-4, highlighting its selectivity and efficacy. This compound is valuable for research applications focused on cancer biology, particularly in the study of signaling pathways and mechanisms associated with EGFR and ErbB receptor activation. -
EGFR ADC
Laprituximab emtansine targets the epidermal growth factor receptor (EGFR) as an antibody-drug conjugate (ADC) incorporating the J2898A antibody linked to DM1, an anti-microtubule agent, via the SMCC thioether linker. This compound exhibits potent anti-cancer activity by delivering cytotoxic agents directly to HER1-expressing cells, thereby enhancing therapeutic efficacy while minimizing systemic toxicity. It is suitable for applications in cancer research, particularly in the study of targeted therapies and EGFR-related pathways. -
EGFR Inhibitor
Rociletinib hydrobromide is a selective inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), particularly effective against the T790M mutation. It demonstrates a Ki value of 21.5 nM for the EGFRL858R/T790M variant, while maintaining a Ki of 303.3 nM for wild-type EGFR. This compound is relevant for research applications aimed at understanding and developing targeted therapies for EGFR-mutant cancers. -
EGFR Inhibitor
Tyrphostin AG 112 is a selective inhibitor of epidermal growth factor receptor (EGFR) phosphorylation. This compound has been shown to interfere with EGFR signaling pathways, resulting in the inhibition of cell proliferation and survival in various cancer cell lines. Tyrphostin AG 112 is utilized in research applications aimed at understanding EGFR-mediated processes and developing targeted therapies for EGFR-associated tumors. -
HER2/EGFR Inhibitor
Neratinib maleate is an orally available, irreversible inhibitor targeting HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively. This compound demonstrates significant anti-tumor activity and is utilized in research for its applications in cancer therapy, particularly in tumors exhibiting overexpression of HER2. Its selective inhibition profile makes it a valuable tool for studies exploring resistance mechanisms and therapeutic efficacy in targeted cancer treatment. -
EGFR-HER2 Inhibitor
Sevabertinib is a potent and reversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values below 0.5 nM for both wild-type HER2 and various mutant forms, including HER2 A775insYVMA, as well as wild-type EGFR and EGFR D770_N771insSVD. This compound demonstrates significant anticancer activity, particularly against lung cancer, making it a valuable tool for research in targeted cancer therapies and signaling pathway studies. -
EGFR/ErbB2 Inhibitor
PD 174265 is a highly selective, reversible inhibitor of the EGFR and ErbB2 tyrosine kinases, demonstrating an IC50 of 0.45 nM. This compound effectively inhibits receptor autophosphorylation and the downstream ERK signaling pathway, leading to significant antitumor activity and reduced toxicity in in vivo models. Additionally, PD 174265 facilitates the differentiation of oligodendrocyte precursor cells, promoting the expression of myelin proteins such as CNP, PLP, and MBP, and enhancing neurite branching. With no inhibitory effect on other kinases like insulin and PDGF receptors, PD 174265 is a vital tool for researching human epidermoid carcinoma treatment and myelin repair mechanisms in multiple sclerosis. -
EGFR/ERBB2 Inhibitor
HKI-357 is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM for EGFR and 33 nM for ERBB2. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, leading to the inhibition of downstream signaling pathways, including AKT and MAPK phosphorylation. HKI-357 is valuable for research into cancer therapies that target these critical signaling pathways. -
IGF-1R Inhibitor
AZ7550 Mesylate is a potent inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), exhibiting an inhibitory concentration (IC50) of 1.6 μM. It is utilized in research to study the role of IGF-1R in cellular signaling pathways, cancer proliferation, and resistance mechanisms. This compound serves as a valuable tool for understanding IGF-1R-related diseases and may aid in the development of targeted therapies. -
FGFR1 Inhibitor
PD-161570 is a potent ATP-competitive inhibitor of the human fibroblast growth factor receptor 1 (FGFR1) with an IC50 of 39.9 nM and a Ki of 42 nM. It also demonstrates inhibitory effects on platelet-derived growth factor receptor (PDGFR), epidermal growth factor receptor (EGFR), and c-Src tyrosine kinases, with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. Additionally, PD-161570 effectively inhibits PDGF-stimulated autophosphorylation and FGFR phosphorylation, with IC50s of 450 nM and 622 nM, respectively. This compound is relevant in studies of bone morphogenetic proteins (BMPs) and TGF-β signaling pathways. -
EGFR Agonist
CN009543V is an agonist of the epidermal growth factor receptor (EGFR) that promotes tyrosine phosphorylation at residues Tyr1068 and Tyr1173, leading to the activation of the MAPK/ERK signaling cascade. Additionally, CN009543V inhibits protein tyrosine phosphatase 1B (PTP-1B) activity in MDA MB468 cancer cells. This compound is applicable in cancer research, particularly in studies focusing on EGFR signaling pathways and their implications in tumor biology. -
EGFR Inhibitor
EGFR-IN-70 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 23.6 nM and 307.5 nM for EGFR-LR/TM/CS and EGFR-WT, respectively. This compound demonstrates significant anti-proliferative effects and effectively suppresses EGFR phosphorylation. EGFR-IN-70 is a valuable tool for cancer research, particularly in studies focusing on EGFR-related signaling pathways and therapeutic interventions. -
EGFR Kinase Inhibitor
PF-06672131 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, targeting the ATP-binding pocket through its alkynylated afatinib derivative structure. This small molecule probe displays reactivity to cysteine and is valuable for activity-based protein profiling studies. Its ability to effectively inhibit EGFR makes it a useful tool in cancer research, particularly in exploring therapeutic strategies for EGFR-driven malignancies. -
EGFR Tyrosine Kinase Inhibitor
Mavelertinib is a highly selective, orally bioavailable irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent inhibitory activity with IC50 values of 5 nM, 4 nM, 12 nM, and 3 nM against Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. This compound is primarily utilized in research related to non-small-cell lung cancer (NSCLC). -
EGFR Inhibitor
Oritinib is an irreversible third-generation inhibitor targeting the epidermal growth factor receptor (EGFR). It effectively overcomes T790M-mediated resistance in non-small cell lung cancer by selectively inhibiting various mutant forms of EGFR, including EGFRWT, EGFRL858R, EGFRL861Q, and both EGFRL858R/T790M and EGFRd746-750 mutations, with low IC50 values ranging from 0.1 to 18 nM. This compound is valuable for research applications focusing on cancer therapeutics and mechanisms of drug resistance. -
Src Inhibitor
β-Hydroxyisovalerylshikonin is a natural product derived from Lithospermum erythrorhizon, functioning as a potent Src inhibitor. It exhibits significant inhibitory activity against protein tyrosine kinases, with IC50 values of 0.7 μM for EGFR and 1 μM for the v-Src receptor. This compound demonstrates broad anticancer activity, particularly inducing cell death in various tumor cell lines, most notably in NCI-H522 and DMS114 cells, making it a valuable tool for cancer research applications. -
EGFR/FLT3/Abl Inhibitor
Ruserontinib is an orally active multikinase inhibitor targeting EGFR, FLT3, and Abl. With an IC50 of 55 nM for human FLT3, it demonstrates significant antitumor activity. This compound is primarily utilized in cancer research, particularly for studying the effects of inhibiting key kinases involved in tumor progression and survival. -
Anti-EGFR/TGFβ Antibody
Ficerafusp alfa is a bispecific antibody targeting EGFR and TGFβ with a Kd of 2.58 nM for EGFR and 61.3 nM for TGFβ1. This compound inhibits EGFR phosphorylation, thereby blocking EGF-dependent cell proliferation and facilitating antibody-dependent cellular cytotoxicity in EGFR-positive tumor cells. Additionally, Ficerafusp alfa sequesters TGFβ via its TGFβRII ECD domain, neutralizing TGFβ activity and inhibiting TGFβ-dependent processes such as epithelial-mesenchymal transition. This reagent is valuable for research on head and neck squamous cell carcinoma, advanced solid tumors, and various cancers including squamous non-small cell lung cancer, anal squamous cell carcinoma, colorectal cancer, and pancreatic cancer. -
EGFR Inhibitor
EGFR-IN-95 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting del19/T790M/C797S and L858R/T790M/C797S mutations. This 2,4-diaminonicotinamide derivative exhibits strong biological activity, making it valuable for research on various EGFR-driven malignancies. Its use is particularly relevant in studies focused on developing targeted therapies for resistant forms of lung cancer and other EGFR-related conditions. -
Mutant-Selective EGFR Inhibitor
Osimertinib-d6 is a deuterium-labeled derivative of osimertinib, a covalent and orally active inhibitor that selectively targets mutant epidermal growth factor receptor (EGFR) variants. With an IC50 of 12 nM against the L858R mutation and 1 nM against L858R/T790M, osimertinib-d6 demonstrates potent efficacy in overcoming T790M-mediated resistance. This compound is valuable for research applications focused on targeted lung cancer therapies and the mechanisms of drug resistance in EGFR-driven tumors. -
EGFR Inhibitor
JCN037 is a non-covalent inhibitor targeting the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity with IC50 values of 2.49 nM for EGFR, 3.95 nM for p-wtEGFR, and 4.48 nM for pEGFRvIII, indicating its effectiveness in inhibiting various EGFR forms. This compound is particularly useful for research applications in cancer biology, especially in studies focused on EGFR signaling pathways and therapeutic resistance mechanisms. Its ability to penetrate the blood-brain barrier further extends its potential in neuro-oncological research. -
EGFR Inhibitor
(E/Z)-AG490 is a racemic mixture of the (E)-AG490 and (Z)-AG490 isomers, functioning as a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates inhibitory activity against other targets, including Stat-3 and the Janus kinases JAK2/3, making it valuable for research in signal transduction and cancer biology. Its ability to modulate key pathways involved in cell proliferation and survival positions (E/Z)-AG490 as an important tool for studying therapeutic strategies in oncology. -
EGFR Inhibitor
EGFR kinase inhibitor 3 is a bivalent ATP-allosteric inhibitor targeting the epidermal growth factor receptor (EGFR) kinase. It demonstrates potent inhibitory activity, with IC50 values of less than 10 nM for wild-type EGFR and as low as 0.059 nM for the L858R/T790M/C797S triple mutant. This compound is particularly useful for studies involving EGFR-mediated signaling pathways and can aid in the development of targeted therapies for EGFR-driven cancers. -
Alflutinib Metabolite/EGFR Inhibitor
AST5902 trimesylate is the primary metabolite of Alflutinib, functioning as an EGFR inhibitor. This compound demonstrates significant antineoplastic activity, making it a valuable reagent for cancer research. Its utility in exploring EGFR-related signaling pathways and therapeutic mechanisms can aid in the development of targeted cancer treatments. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 8 (T-184) is a proteolysis-targeting chimera (PROTAC) that specifically degrades the epidermal growth factor receptor (EGFR). With a DC50 of 15.56 nM in HCC827 cells, it effectively reduces EGFR levels and demonstrates potent growth inhibition in H1975, PC-9, and HCC827 cell lines, exhibiting IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is valuable for research focusing on cancer biology, particularly non-small cell lung cancer (NSCLC). -
EGFR Activator
13(S)-HPODE is a linoleic acid metabolite that acts as an EGFR activator. It has demonstrated significant biological activity in promoting cell proliferation and may play a role in various signaling pathways associated with cancer progression and inflammation. This compound is valuable for research into mechanisms of cancer biology and the development of therapeutic strategies targeting the EGFR pathway. -
EGFR-TKI Inhibitor
PKI-166 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating potent activity with an IC50 of 0.7 nM. It exhibits oral bioavailability and is utilized in research focused on cancer therapies that target aberrant EGFR signaling pathways. PKI-166 serves as a valuable tool for investigating the role of EGFR in tumorigenesis and evaluating the efficacy of EGFR-targeted treatments in various cancer models. -
EGFR/ErbB2 Inhibitor
Selatinib is a reversible and orally bioavailable dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2, demonstrating IC50 values of 13 nM and 22.5 nM, respectively. This compound exhibits significant anticancer activity, making it a valuable tool for research in targeted cancer therapies and studies focused on EGFR and ErbB2 signaling pathways.
