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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR/HER2 Inhibitor
EGFR/HER2-IN-11 is a potent dual inhibitor targeting the human epidermal growth factor receptors HER2 and EGFR, demonstrating IC50 values of 7.7 nM and 22 nM, respectively. This compound exhibits significant antitumor activity and effectively inhibits the proliferation of cancer cells, specifically showing a GI50 of 601 nM against the BT-474 cell line. EGFR/HER2-IN-11 is suitable for research applications focused on cancer biology and therapeutic development targeting these key oncogenes. -
EGFR Inhibitor
CGP-59326 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 0.027 μM. This compound effectively disrupts the EGFR signaling pathway, exhibiting strong inhibition of EGFR-dependent tumor cells. CGP-59326 is valuable for research applications in cancer biology, particularly in studies investigating EGFR-related malignancies. -
EGFR Inhibitor
EGFR-IN-71 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 3.7 μM. This compound is particularly useful in research focused on chordoma, providing a tool for studying EGFR-related signaling pathways. Additionally, EGFR-IN-71 features an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling diverse applications in chemical biology and bioconjugation studies. -
EGFR Inhibitor
EGFR-IN-193 is an inhibitor of the Epidermal Growth Factor Receptor (EGFR), primarily utilized in the synthesis of PROTACs as target protein ligands. It serves as a crucial component in the development of novel protein degradation strategies, particularly exemplified by PROTAC EGFR degrader 17, facilitating studies in cancer biology and targeted therapy research. This compound enables the exploration of EGFR signaling pathways and their roles in oncogenesis and tumor progression. -
EGFR-C797S Inhibitor
EGFR/C797S-IN-1 is a selective inhibitor targeting the EGFR-C797S variant, demonstrating an IC50 of 0.128 µM. This compound exhibits significant anti-proliferative and anti-tumor effects, making it a valuable tool for cancer research. Notably, EGFR/C797S-IN-1 inhibits the phosphorylation of EGFR in a dose-dependent manner, contributing to its potential in therapeutic applications against resistant tumor phenotypes. -
EGFR Inhibitor
HG-5-88-01 is an EGFR inhibitor that disrupts epidermal growth factor receptor signaling pathways. It demonstrates notable anti-cancer activity independent of EGFR expression levels, making it a valuable tool for exploring therapeutic resistance mechanisms. This compound is particularly relevant for research in cancer biology and the development of alternative therapies targeting EGFR. -
EGFR Inhibitor
EGFR-IN-167 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.19 nM. This compound demonstrates high potency against various EGFR mutants, with IC50 values of 0.109 nM for EGFR (L858R), 0.75 nM for EGFR (C797S), and <0.05 nM for EGFR (del19). EGFR-IN-167 covalently binds to the catalytically conserved lysine residue in EGFR within live mammalian cells, effectively inhibiting EGFR autophosphorylation and showing significant anti-proliferative activity. This reagent is valuable for research in non-small-cell lung carcinomas (NSCLC), glioblastoma, and other solid tumors. -
EGFR Inhibitor
EGFR kinase inhibitor 4 is a bivalent ATP-allosteric inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 1.8 nM specifically for the mutant EGFR variant (LRTMCS). This compound is primarily utilized in research focused on non-small cell lung cancer (NSCLC), providing insights into EGFR-related signaling pathways and therapeutic resistance mechanisms. -
EGFR Tyrosine Kinase Inhibitor
EGFR-IN-87 is an EGFR tyrosine kinase inhibitor that demonstrates potent inhibition with IC50 values of 3.1 nM, 1.3 nM, and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790, and wild-type EGFR in A431 cells, respectively. This compound is valuable for investigating EGFR-related signaling pathways and is applicable in cancer research, particularly in the context of targeted therapies for tumors expressing mutated forms of the receptor. -
EGFR Mutant Inhibitor
EGFR mutant-IN-2 (Compound D51) is a selective inhibitor targeting the EGFR mutant variants, specifically EGFRL858R/T790M/C797S and EGFRdel19/T790M/C797S, with IC50 values of 14 nM and 62 nM, respectively. This compound demonstrates significant antitumor activity alongside favorable pharmacokinetic properties and in vivo stability, making it a valuable tool for research in cancer therapeutics. Its ability to effectively inhibit challenging EGFR mutations underscores its potential application in studying resistance mechanisms and developing targeted treatments. -
EGFR Kinase Inhibitor
Erlotinib-d6 hydrochloride is a deuterium-labeled inhibitor of the epidermal growth factor receptor (EGFR) kinase, demonstrating potent inhibition with an IC50 of 2 nM. This compound serves as a valuable tool in chemical research, particularly in the study of EGFR-related signaling pathways in cancer. Additionally, Erlotinib-d6 hydrochloride features an alkyne group, enabling its application in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the labeling and tracking of biomolecules containing azide groups. -
EGFR Allosteric Inhibitor
JBJ-04-125-02 is a potent allosteric inhibitor of the epidermal growth factor receptor (EGFR), demonstrating selective activity against mutant forms, particularly EGFRL858R/T790M, with an IC50 of 0.26 nM. This compound effectively inhibits the proliferation of cancer cells and disrupts signaling pathways associated with EGFRL858R/T790M/C797S mutations. JBJ-04-125-02 exhibits significant anti-tumor properties, making it a valuable tool for research in targeted cancer therapies. -
SOS1/EGFR Inhibitor
SOS1/EGFR-IN-1 is a dual-target inhibitor that specifically targets SOS1 and EGFR, demonstrating IC50 values of 42.13±1.55 nM and 1.01±0.04 nM, respectively. This compound effectively induces apoptosis and G1 phase cell cycle arrest, while reducing angiogenesis and cell migration. SOS1/EGFR-IN-1 exhibits significant antitumor activity in prostate cancer cells, with an IC50 of 0.45±0.03 μM, making it a valuable tool for research in cancer therapies. -
EGFR Inhibitor
4-Methyl erlotinib is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound effectively disrupts EGF-mediated tumor cell proliferation by significantly lowering EGFR-specific tyrosine phosphorylation levels. In preclinical studies utilizing a mouse model of human tumor transplantation, 4-Methyl erlotinib exhibited notable and prolonged inhibition of EGFR phosphotyrosine levels, leading to substantial growth inhibition in EGFR-dependent human malignancies. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-9 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It demonstrates inhibitory activity with IC50 values of 3.2 nM against EGFR, 8.3 nM against the EGFR T790M mutant, and 14 nM against HER2. This compound is applicable in research focused on targeted cancer therapies, particularly for tumors exhibiting dysregulated EGFR and HER2 signaling pathways. -
EGFR Inhibitor
EGFR-IN-85 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 0.19 μM for EGFRvIII phosphorylation. This compound effectively suppresses EGFR signaling within tumor microenvironments, making it a valuable tool for studying glioblastoma (GBM) and related malignancies. Researchers can utilize EGFR-IN-85 to elucidate the role of EGFR in tumor progression and to explore potential therapeutic interventions. -
EGFR Inhibitor
YS-67 is a highly effective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 5.2 nM. This compound significantly reduces the phosphorylation of EGFR and AKT, indicating its potential to disrupt downstream signaling pathways. YS-67 demonstrates notable antiproliferative effects on human cancer cell lines, including A549, PC-9, and A431, with IC50 values of 4.1 μM, 0.5 μM, and 2.1 μM, respectively. This makes YS-67 a valuable reagent for research focused on therapeutic strategies targeting EGFR in various cancer models. -
EGFR L858R/T790M Mutant Inhibitor
EGFR-IN-1 TFA is an irreversible inhibitor targeting the EGFR L858R/T790M mutant, specifically designed to overcome resistance to Gefitinib. It demonstrates exceptional potency, exhibiting a 100-fold selectivity over wild-type EGFR. This compound shows robust antiproliferative effects against H1975 and HCC827 cell lines, highlighting its potential for antitumor applications in the treatment of lung cancer driven by these mutations. -
EGFR Inhibitor
EGFR-IN-69 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating potent activity with IC50 values of 4.3 nM for EGFRL858R/T790M/C797S, 6.6 nM for EGFRL858R/T790M, and 25.6 nM for EGFR19del/T790M/C797S. This compound is particularly relevant for research in non-small-cell lung cancer (NSCLC), providing valuable insights into therapeutic strategies targeting mutant EGFR variants. Its efficacy in inhibiting EGFR activity makes it an important tool for advancing cancer research and drug development. -
EGFR/ErbB2 Inhibitor
GW583340 dihydrochloride is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and ErbB2 tyrosine kinases, with IC50 values of 0.01 μM and 0.014 μM, respectively. This compound effectively reverses drug resistance mediated by ABCG2 and ABCB1 transporters, enhancing the efficacy of chemotherapeutic agents. GW583340 dihydrochloride demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer biology and therapeutic development. -
EGFR Inhibitor, Estrogen Receptor Inhibitor, Progesterone Receptor Inhibitor
4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions. -
EGFR Inhibitor
Tyrosine kinase-IN-7 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It exhibits inhibitory activity with IC50 values of 0.630 μM for EGFR wild-type and 0.956 μM for the T790M mutant variant. Tyrosine kinase-IN-7 demonstrates significant antitumor effects across several cancer cell lines, including HepG2, HCT-116, MCF-7, and A431, with respective IC50 values of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM. This compound is useful for research focused on cancer therapeutics targeting the EGFR signaling pathway. -
EGFR-T790M Inhibitor
ES-072 is a selective inhibitor of the EGFR-T790M mutation, primarily targeting this mutant receptor to activate GSK3α. By inhibiting EGFR-T790M activity, ES-072 promotes the phosphorylation of PD-L1 at Ser279 and Ser283, which facilitates its ubiquitination and subsequent proteasomal degradation via the E3 ligase ARIH1. This dual mechanism not only suppresses cancer cell proliferation but also enhances the anti-tumor immune response through reduced PD-L1 expression. ES-072 is applicable in research focused on non-small cell lung cancer (NSCLC) treatment strategies. -
EGFR Inhibitor
BPI-15086 is an orally active, potent, irreversible inhibitor targeting the epidermal growth factor receptor (EGFR) and specifically the T790M resistance mutation. This compound exhibits significant biological activity against mutant EGFR, making it a valuable tool for research focused on non-small-cell lung cancer. Its selective action aids in the study of resistance mechanisms and therapeutic responses associated with EGFR mutations. -
EGFR Inhibitor
Derazantinib dihydrochloride is a potent inhibitor of the fibroblast growth factor receptor (FGFR) family, specifically targeting FGFR1, FGFR2, and FGFR3 with IC50 values of 4.5 nM, 1.8 nM, and 2.4 nM, respectively. Its mechanism involves competitive inhibition of ATP binding, which effectively reduces FGFR phosphorylation. This compound has demonstrated significant anti-tumor effects in various xenograft models, making it valuable for research in cancer biology and targeted therapies. -
EGFR Inhibitor
Theliatinib tartrate is a potent, ATP-competitive inhibitor of the epidermal growth factor receptor (EGFR) with a Ki of 0.05 nM and an IC50 of 3 nM. This compound demonstrates an IC50 of 22 nM for EGFR T790M/L858R mutants and exhibits over 50-fold selectivity for EGFR compared to other kinases. Additionally, Theliatinib tartrate contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it useful for click chemistry applications in research. -
EGFR Inhibitor
Dosimertinib-d3 is a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound effectively reduces levels of phosphorylated EGFR and ERK proteins, exhibiting significant antiproliferative and antitumor activities. Dosimertinib-d3 is particularly relevant for research applications targeting non-small-cell lung cancer (NSCLC) and offers a valuable tool for studying EGFR-mediated signaling pathways. -
EGFR Allosteric Inhibitor
JBJ-02-112-05 is a potent allosteric inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting mutant forms such as EGFRL858R/T790M with an IC50 of 15 nM. This compound offers a selective approach to inhibit aberrant EGFR activity, making it valuable for research applications in cancer therapeutics and precision oncology. Its oral bioavailability further enhances its utility in preclinical studies of EGFR-driven tumors. -
EGFR/HER2 Inhibitor
Mobocertinib mesylate is an orally active and irreversible inhibitor of EGFR and HER2. It exhibits potent inhibition of oncogenic variants with activating EGFR exon 20 insertion mutations while showing selectivity for wild-type EGFR. This reagent is primarily utilized in research focused on non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR/CSC-IN-1 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 10.52 nM, and it also targets cancer stem cells (CSCs). This dual inhibition is particularly relevant for research focused on triple-negative breast cancer, offering a pathway to explore therapeutic strategies that may improve treatment outcomes in this aggressive malignancy. -
EGFR Inhibitor
EGFR-IN-31 is a selective inhibitor of the epidermal growth factor receptor (EGFR), a key protein implicated in the regulation of cell proliferation and survival. The overexpression and mutation of EGFR are linked to various cancers, particularly non-small cell lung cancer (NSCLC). This compound is designed for research focused on the role of EGFR mutations in disease progression and may aid in the development of targeted therapies for EGFR-related malignancies. -
EGFR Inhibitor
Oritinib mesylate is a selective, orally active irreversible inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 18 nM. This compound demonstrates strong activity against both EGFR-sensitive and T790M-resistant mutations. Oritinib mesylate effectively inhibits the proliferation of tumor cells harboring these mutations, making it a valuable tool for research in cancer biology and targeted therapies. -
EGFR Inhibitor
EGFR-IN-103 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 6 nM for phosphorylated EGFR (pEGFR). This compound demonstrates effective inhibition of EGFR-mediated signaling pathways, making it valuable in cancer research, particularly in drug resistance studies and therapeutic applications targeting EGFR-driven tumors. Its specificity and potency make it an essential tool for studying EGFR-related biological processes and evaluating new therapeutic strategies. -
EGFR Triple Mutant Inhibitor
EMI48 is a selective inhibitor targeting the EGFR triple mutant variant. It exhibits enhanced potency compared to its predecessor, EMI1, effectively inhibiting the activity of mutant EGFR. This compound is valuable for research focused on understanding the mechanisms of resistance in cancer therapy and evaluating therapeutic strategies against EGFR-mutant tumors. -
EGFR Inhibitor
EGFR-IN-15 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 4 nM. This compound is pivotal for research in oncological diseases, allowing for the exploration of EGFR signaling pathways and their role in tumorigenesis. Its high specificity and efficacy make it a valuable tool for therapeutic investigations and drug development targeting EGFR-driven malignancies. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-2 is a dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It demonstrates potent inhibitory activity with IC50 values of 5.02 µM for EGFR and 0.83 µM for HER2. This compound is valuable for research applications focusing on cancer biology, particularly in the study of EGFR and HER2 signaling pathways and their role in tumor proliferation and resistance mechanisms. -
EGFR Inhibitor
BI-8128 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 12 nM for wild-type and 3 nM for the L858R/T790M/C797S mutant variants. This compound effectively inhibits the proliferation of Ba/F3 and PC-9 cells that are resistant to conventional therapies. BI-8128 is particularly relevant for research focused on non-small cell lung cancer, providing valuable insights into resistance mechanisms and potential therapeutic strategies. -
EGFR Inhibitor
EGFR-IN-36 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 19.09 nM, 120.01 nM, and 2.35 nM for wild-type EGFR, wild-type HER2, and the HER2 mutant A775_G776insYVMA, respectively. This compound demonstrates significant potential in research focused on tumor types driven by both wild-type and mutant forms of EGFR and HER2 kinases, making it a valuable tool for investigating targeted cancer therapies. -
EGFR Inhibitor
EGFR-IN-25 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 9 nM in BaF3 cells harboring the EGFR DEL19/T790M/C797S mutation and 60 nM in A431 cells expressing wild-type EGFR. This compound exhibits significant biological activity that supports its application in cancer research, particularly in studies targeting EGFR-driven tumors. EGFR-IN-25 can be utilized to investigate the effects of EGFR inhibition on cell proliferation and survival in relevant preclinical models. -
EGFR Inhibitor
Rezivertinib hydrochloride is a highly selective and irreversible third-generation inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates potent activity against both the common EGFR activating mutations and the T790M resistance mutation. This compound also possesses excellent central nervous system (CNS) penetration, making it a valuable tool in the study of antitumor activity, particularly in the context of non-small cell lung cancer (NSCLC). Researchers may utilize Rezivertinib hydrochloride to investigate mechanisms of resistance and evaluate therapeutic strategies targeting EGFR-related pathways. -
EGFR inhibitor
EGFR-IN-24 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrated to effectively target both EGFR mutations del19/T790M/C797S and L858R/T790M/C797S. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research, particularly for studies focused on non-small cell lung cancer and resistance mechanisms associated with EGFR mutations. Researchers can utilize EGFR-IN-24 to explore therapeutic strategies and develop potential treatment options for patients harboring these challenging mutations. -
EGFR Inhibitor
Tyrphostin AG30 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It effectively inhibits self-renewal induction mediated by c-ErbB and obstructs the activation of STAT5 by c-ErbB in primary erythroblasts. This compound serves as a valuable tool in cancer research, particularly in studies focused on EGFR signaling pathways and their role in tumor proliferation and growth. -
EGFR Inhibitor
EMI1 is a selective inhibitor of mutant epidermal growth factor receptor (EGFR) variants, specifically ex19del/T790M/C797S and L858R/T790M/C797S. This compound demonstrates significant efficacy against drug-resistant non-small-cell lung cancer (NSCLC) associated with these mutations. EMI1 serves as a valuable tool for research investigating the molecular mechanisms of EGFR-related resistance and potential therapeutic strategies in NSCLC. -
EGFR Inhibitor
Afatinib impurity 11 is an impurity associated with Afatinib, a well-known irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. Afatinib exhibits potent biological activity, with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM against wild-type EGFR, EGFRL858R, EGFRL858R/T790M, and HER2, respectively. This compound is essential for investigating the purity and synthesis of Afatinib, contributing to research focused on targeted cancer therapies. -
EGFR Inhibitor
Erlotinib-d6 is a deuterated analog of Erlotinib, specifically targeting the epidermal growth factor receptor (EGFR) as a tyrosine kinase inhibitor. With an IC50 of 2 nM for human EGFR, it demonstrates potent inhibitory activity crucial for studying EGFR-mediated signaling pathways. As a click chemistry reagent, Erlotinib-d6 contains an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) for applications in chemical biology and bioconjugation research. -
EGFR Inhibitor
EGFR-IN-122 is a potent inhibitor of the epidermal growth factor receptor (EGFR), a critical target in cancer therapy. This compound effectively suppresses the proliferation of EGFR-driven cancer cell lines, specifically PC-9GR and HCC827GR. Its use in research applications contributes to the understanding of EGFR signaling pathways and aids in the development of targeted therapies for EGFR-dependent tumors. -
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 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.
