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EGFR and HER2 inhibitors act on two closely related receptor tyrosine kinases of the ErbB family. The epidermal growth factor receptor (EGFR, ErbB1) and human epidermal growth factor receptor 2 (HER2, ErbB2) form dimers with each other and with ErbB3 and ErbB4. Receptor activation engages the mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K) pathways that control cell growth. Activating EGFR mutations in non-small-cell lung cancer have made the receptor a central model in kinase inhibitor research. Gefitinib and erlotinib are reversible EGFR inhibitors, and lapatinib inhibits both EGFR and HER2. Osimertinib binds covalently to EGFR carrying the T790M resistance mutation, and neratinib irreversibly inhibits HER2 and EGFR.
TAS2940 is a selective, irreversible pan-ERBB inhibitor that effectively penetrates the blood-brain barrier. It exhibits significant inhibitory activity against wild-type HER2, HER2 V777L, and A775_G776insYVMA, with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. This compound is applicable for research focused on tumors exhibiting HER2 and EGFR aberrations, providing valuable insights into targeted cancer therapies.
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EGFR-IN-177 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.32 nM against the EGFR L858R mutation and 0.67 nM against EGFR D746-750, among others. This compound effectively inhibits lung cancer cell proliferation and the phosphorylation of EGFR, demonstrating significant potential for therapeutic applications in non-small cell lung cancer research. EGFR-IN-177 is a valuable tool for exploring mechanisms of resistance and sensitivity in targeted cancer therapies.
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EGFR-IN-126 is a potent inhibitor targeting the EGFRL858R/T790M/C797S mutations, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant antitumor activity in both in vivo and in vitro models, making it a valuable tool for cancer research and therapeutic development focusing on EGFR-related malignancies.
EGFR/HER2-IN-4 is an irreversible dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits potent inhibition of EGFR with an IC50 of 0.6 nM and effectively inhibits kinase activity associated with L858R and T790M mutations. Demonstrating significant antitumor efficacy in vivo, EGFR/HER2-IN-4 is a valuable reagent for research on lung cancer and related therapeutic strategies.
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EGFR-IN-203 is a selective inhibitor of the EGFR kinase domain, specifically targeting the mutant forms EGFRT790M, C797S, and V948R. It exhibits a stable binding affinity to the allosteric pocket of EGFR in its inactive conformation. This compound is valuable for research applications focused on cancer, particularly non-small cell lung cancer, providing insights into EGFR-related pathways and potential therapeutic strategies.
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EGFR T790M/L858R-IN-5 is a selective inhibitor targeting the EGFR T790M and L858R mutations. It demonstrates a high inhibition percentage of 92.9% at a concentration of 0.05 μM, making it a valuable tool for research into targeted cancer therapies. This compound is primarily utilized in studies aimed at understanding resistance mechanisms in non-small cell lung cancer and the development of effective treatment strategies.
EGFR-IN-42 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating single-digit nanomolar activity. This compound forms a covalent linkage between tamoxifen or endoxifen and the EGFR inhibitor gefitinib, allowing it to retain both estrogen receptor antagonist and EGFR inhibitory properties. EGFR-IN-42 shows enhanced anti-cancer activity, making it a valuable tool for research into dual-target therapeutic strategies in cancer treatment.
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EGFR-IN-68 is a selective inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.33 μM. This compound demonstrates significant anticancer activity, making it valuable for research on tumor proliferation and metastasis. It is particularly useful in studies examining EGFR signaling pathways and developing targeted therapeutic strategies in cancer biology.
EGFR-IN-55 is a selective inhibitor of the Epidermal Growth Factor Receptor (EGFR), exhibiting potent activities with IC50 values of 70 nM for wild-type EGFR and 3.9 nM for the EGFRL858R/T790M mutant. This compound effectively induces cell cycle arrest in the G0/G1 phase in NCI-H1975 cells, demonstrating significant anticancer activity. EGFR-IN-55 is a valuable tool for research in cancer biology, particularly in studies targeting EGFR-related pathways.
Synonyms: AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875
Tyrphostin 25 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating an IC50 of 3 µM in A431 cells. Additionally, this compound acts as an agonist for GPR35, exhibiting an EC50 of 5.3 µM. Tyrphostin 25 is utilized in research applications focused on cancer biology and signal transduction pathways, making it a valuable tool for understanding EGFR-related mechanisms and GPR35 function.
RG-14467 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exerting its action by inhibiting enzymatic activity. It exhibits inhibition kinetics comparable to Lavendustin-A, with a dissociation constant of 3.4 μM for the rapidly formed initial complex and an overall dissociation constant estimated at 30 nM or less. RG-14467 functions as a partially competitive inhibitor of ATP, making it a valuable tool for research applications focused on EGFR-related signaling pathways and cancer therapeutics.
EGFR/HER2-IN-3 is a potent dual inhibitor targeting epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits significant biological activity in inhibiting cell proliferation and tumor growth associated with EGFR and HER2 overexpression. This compound is particularly useful in cancer research, facilitating studies on therapeutic interventions for tumors driven by these pathways.
EGFR-IN-39 is a potent inhibitor of the epidermal growth factor receptor (EGFR), a pivotal target in the regulation of cell proliferation. This acrylamide derivative exhibits significant anti-tumor activity with minimal associated toxicity, making it a valuable candidate for cancer research, particularly concerning non-small cell lung cancer (NSCLC). Given its ability to address conditions linked to EGFR overexpression and mutations, EGFR-IN-39 holds promise for advancing the understanding and treatment of EGFR-driven malignancies.
EGFR-IN-29 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates significant biological activity in blocking EGFR signaling pathways, which are critical in various tumorigenic processes. EGFR-IN-29 is useful in research applications focused on cancer biology and therapeutic resistance, providing insights into targeted therapy for EGFR-driven malignancies.
EGFR-IN-114 is a selective non-covalent inhibitor targeting mutant forms of the epidermal growth factor receptor (EGFR). Demonstrating potent inhibitory activity, it is primarily utilized in research focused on non-small cell lung cancer (NSCLC). This compound provides a valuable tool for studying EGFR signaling pathways and developing targeted therapies in oncological research.
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EGFR-IN-133 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively targeting various mutations including wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with IC50 values of 0.1, 0.044, 0.036, 0.04, and 0.054 nM, respectively. This compound demonstrates favorable pharmacokinetic properties and exhibits high oral bioavailability, making it a useful tool in molecular biology and cancer research for studying EGFR signaling pathways and developing targeted therapies for EGFR-mutant cancers.
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EGFR-IN-37 is a selective inhibitor of epidermal growth factor receptor (EGFR), designed to target and disrupt its activity. This compound exhibits significant anti-tumor effects while minimizing toxic side effects, making it suitable for therapeutic research. Given the role of EGFR overexpression and mutations in driving uncontrolled cell proliferation, particularly in non-small cell lung cancer (NSCLC), EGFR-IN-37 presents a valuable tool for investigating EGFR-related malignancies. Its applications extend to the study of disease mechanisms and potential treatment strategies for conditions associated with EGFR mutations.
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EGFR-IN-200 is a selective inhibitor of the epidermal growth factor receptor (EGFR), with IC50 values of 0.03 μM for EGFR, 3.1 μM for TNF-α, and 1.6 μM for the IL-6/GP130 complex. By binding to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, it induces G2/M cell cycle arrest, apoptosis, and demonstrates potent antiproliferative activity. With high gastrointestinal absorption and low blood-brain barrier permeability, EGFR-IN-200 is valuable for investigating mechanisms in lung cancer and breast adenocarcinoma research.
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EGFR-IN-110 is a covalent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR-expressing cells. This compound demonstrates robust inhibitory activity against EGFR, coupled with favorable selectivity for kinases. It serves as a valuable tool in research focused on targeting EGFR-related pathways and exploring therapeutic interventions in EGFR-driven cancers.
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EGFR-IN-157 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 18.81 nM. This compound is primarily utilized in research focused on non-small cell lung cancer (NSCLC), enabling investigations into EGFR-mediated signaling pathways and therapeutic strategies. Its efficacy in inhibiting EGFR activity makes it a valuable tool for studying the molecular mechanisms underlying NSCLC and developing targeted cancer therapies.
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Emupertinib is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of less than 0.3 nM for the EGFR d746-750/T790M/C779S mutant and up to 0.92 nM for wild-type EGFR. This compound effectively inhibits various EGFR mutations, including L858R/T790M/C797S and d746-750/C797S, making it a valuable tool for research on targeted therapies in cancer treatment. Its high specificity and efficacy position Emupertinib as a significant candidate for studying EGFR-related signaling pathways and developing novel anticancer agents.
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EGFR-IN-22 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating potent activity with IC50 values of 4.91 nM for wild type EGFR and 0.54 nM for the mutant variants EGFR L858R/T790M/C797S. This compound is valuable for preclinical research aimed at understanding the role of EGFR signaling in various cancers, particularly those harboring specific mutations associated with resistance to standard therapies.
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EGFR-IN-38 is a selective inhibitor of the epidermal growth factor receptor (EGFR), which plays a critical role in cancer cell proliferation. This compound exhibits significant anti-tumor activity while maintaining low toxicity, making it a valuable tool in cancer research. Its mechanism of action addresses the overexpression and mutations of EGFR, commonly implicated in the development and progression of various malignancies, particularly non-small cell lung cancer (NSCLC). EGFR-IN-38 serves as a promising candidate for investigating EGFR-related pathologies and therapeutic strategies.
EGFR/HER2-IN-7 is a selective inhibitor targeting the EGFR and HER2 kinases, demonstrating potent antitumor activity in MCF-7 breast cancer cells. With IC50 values of 0.18 μM for EGFR and 0.146 μM for HER2, it effectively impedes signaling pathways involved in cancer progression. Additionally, EGFR/HER2-IN-7 exhibits moderate inhibition of dihydrofolate reductase (DHFR) with an IC50 of 0.907 μM. This compound is relevant for research focused on therapeutic strategies for breast cancer and the modulation of related signaling pathways.
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EGFR-IN-81 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting both wild-type and mutant forms (L858R/T790M) with IC50 values of 4.38 nM and 5.69 nM, respectively. This compound exhibits significant cytotoxic effects on cancer cell lines, demonstrating inhibitory concentrations of 2.07 μM against MCF-7 cells and 6.72 μM against HCT116 cells. EGFR-IN-81 is useful for research applications focused on cancer biology and therapeutic development targeting EGFR-driven malignancies.
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