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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.
EGFR T790M/L858R-IN-6 is a pyrimidine-based inhibitor specifically targeting the EGFR mutations T790M and L858R. This compound demonstrates potent inhibitory activity, achieving 90.88% inhibition of enzyme activity at a concentration of 0.05 μM. It serves as a valuable tool for research focused on the development of targeted therapies for EGFR-mutant cancers.
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Nelipepimut-S is a peptide vaccine that specifically targets the HER2 protein, which is overexpressed in certain breast cancers. This vaccine activates the immune system, promoting a targeted response against HER2-positive tumors. Nelipepimut-S is utilized in research focused on developing immunotherapies for breast cancer treatment and understanding the mechanisms of immune modulation in tumor environments.
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UNC-CA359 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 18 nM. This compound exhibits significant anti-tumor activity and is particularly applicable in chordoma research. Additionally, UNC-CA359 features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool in click chemistry applications.
EGFR-IN-136 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 20.2 nM for EGFRWT, 1.2 nM for EGFRLR/TM, 2.3 nM for EGFR19D/TM/CS, and 12.5 nM for EGFRLR/TM/CS. This compound exhibits significant antiproliferative and antitumor activity, making it a valuable tool for research involving non-small cell lung cancer (NSCLC). Its selective inhibition of various EGFR mutations positions EGFR-IN-136 as an important reagent for investigating therapeutic strategies targeting EGFR-related pathways.
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EGFR-IN-145 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase. At a concentration of 20 μM, it demonstrates a 52.7% inhibition of EGFR-wild type kinase activity. This compound is valuable for research in cancer biology, particularly in the study of oncogenic signaling pathways and the development of targeted therapies for EGFR-driven tumors.
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is a phosphorylated peptide that serves as a substrate for the epidermal growth factor receptor (EGFR). This product is utilized for the evaluation of EGFR kinase inhibitors through the quantification of phosphorylated substrates, aiding in the exploration of signaling pathways and potential therapeutic applications in cancer research. Its precise autophosphorylation site makes it an essential tool for discerning kinase activity in various biological assays.
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NSC81111 is a potent orally active inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK), demonstrating an IC50 of 0.15 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its efficacy in targeting EGFR pathways positions NSC81111 as a promising candidate for studies focused on cancer therapeutics and mechanisms of resistance.
Synonyms: NEP010
Neptinib is an orally active derivative of Afatinib, primarily targeting the EGFR kinase family. It demonstrates enhanced antitumor activity compared to its predecessor, attributed to improved pharmacokinetics. Notably, Neptinib significantly inhibits tumor growth in mouse models of non-small cell lung cancer harboring various EGFR mutations, with IC50 values of 0.24 nM for EGFRwt, 7.25 nM for EGFRL858R/T790M, 0.46 nM for EGFRL858R, and 1.79 nM for EGFRT790M. This compound is valuable for research focused on targeted cancer therapies and the study of EGFR-related pathologies.
Paeciloquinone D is an inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It exhibits significant biological activity by blocking EGFR signaling pathways, which are critical in tumor growth and proliferation. This compound is relevant for research applications focused on cancer biology and targeted therapies for EGFR-driven malignancies.
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BML-265 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It disrupts Golgi integrity and inhibits the secretory transport of various protein cargos in human cells, but shows no effect in rodent cells. This specificity makes BML-265 a valuable tool for studying EGFR signaling pathways and Golgi function in human cellular contexts.
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Tyrphostin 63 is a selective inhibitor of the epidermal growth factor receptor (EGFR). Exhibiting an IC50 value of 375 μM and a Ki value of 123 μM, Tyrphostin 63 effectively modulates EGFR signaling pathways. This compound is primarily utilized in cancer research to investigate the role of EGFR in tumor proliferation and metastasis.
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EGFR-IN-149 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.42 nM. This compound effectively blocks EGFR signaling, which is crucial in regulating cellular proliferation and survival. Its prominent biological activity makes it a valuable tool for research applications focused on cancer therapies, particularly in studies involving EGFR-dependent tumor growth and resistance mechanisms.
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EGFR-IN-146 is an inhibitor of the epidermal growth factor receptor (EGFR) that disrupts EGFR signaling, effectively enhancing insulin sensitivity through AMPK pathway activation. This compound exhibits significant potential in reducing blood glucose levels and body weight. EGFR-IN-146 is valuable for research applications focused on diabetes and obesity, offering insights into metabolic regulation and potential therapeutic options.
DDC4002 is a selective inhibitor of the epidermal growth factor receptor (EGFR), targeting the L858R/T790M mutant subtype with an IC50 of 39 nM. This compound exhibits potent inhibitory activity, making it a valuable tool for cancer research, particularly in studies focused on therapeutic resistance in non-small cell lung cancer. Its application supports investigations into the mechanisms of EGFR-driven malignancies and offers insights into potential treatment strategies.
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Paeciloquinone E is a selective inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. This compound demonstrates significant biological activity in modulating cell proliferation and survival pathways associated with EGFR signaling. It serves as a valuable tool in cancer research, particularly for studying the effects of EGFR inhibition in various tumor models.
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EGFR ligand-11 is a specific ligand for the epidermal growth factor receptor (EGFR). This compound plays a crucial role in synthesizing PROTAC MS154, facilitating targeted protein degradation of EGFR-related pathways. It is valuable for research applications focused on understanding EGFR signaling and developing therapeutic strategies for EGFR-driven cancers.
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NRC-2694-A is a potent orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It exhibits significant activity against malignant squamous cell carcinoma (HNSCC), making it a valuable tool for researchers investigating EGFR-related signaling pathways and therapeutic strategies in cancer treatment. Its application in preclinical studies may enhance understanding of tumorigenesis and resistance mechanisms associated with EGFR inhibition.
PF-6422899 is a selective inhibitor of the epidermal growth factor receptor (EGFR) that exhibits binding affinity in the nanomolar range. It demonstrates potent biological activity against EGFR, making it a valuable tool in cancer research, particularly in studies focused on EGFR-driven pathways. Additionally, PF-6422899 may also interact with SOAT1, suggesting potential applications in the modulation of lipid metabolism in cancer cells.
HKI-357 dimaleate is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM and 33 nM, respectively. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, as well as the phosphorylation of downstream signaling molecules AKT and MAPK. HKI-357 dimaleate is primarily used in research to investigate mechanisms of oncogenesis and assess potential therapeutic strategies in cancer that involve EGFR and ERBB2 pathways.
Paeciloquinone F is a potent inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It has been demonstrated to effectively impede EGFR signaling pathways, making it a valuable tool for studies focused on cancer research and therapeutic development. The compound's ability to modulate EGFR activity facilitates investigations into tumor growth and progression, as well as the potential for targeted cancer therapies.
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Paeciloquinone C is a potent inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It effectively inhibits the V-abl protein tyrosine kinase with an IC50 value of 0.56 μM. This compound is utilized in research focused on cancer biology and targeted therapies, providing insights into the mechanisms of EGFR-mediated signal transduction.
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Synonyms: AFN-941
1,2,3,4-Tetrahydro Staurosporin is a selective inhibitor of the mutant epidermal growth factor receptor (EGFR), particularly EGFRT790M, with an IC50 of 74 nM, demonstrating potential in targeting drug-resistant mutations. This compound also exhibits a higher IC50 of 390 nM against wild-type EGFR, highlighting its specificity. Additionally, 1,2,3,4-Tetrahydro Staurosporin interacts with Janus kinase 3 (JAK3), making it suitable for research applications focused on cancer biology and signaling pathways.
EGFR-IN-99 is a potent inhibitor specifically targeting EGFR and HER2 Exon 20 insertion mutants. This compound exhibits exceptional antiproliferative activity in DFCI127 cells, with an EC50 value of 11.5 nM. EGFR-IN-99 is designed for research applications related to non-small cell lung cancer (NSCLC), making it a valuable tool for studying mutant-driven tumorigenesis and therapeutic resistance.
Paeciloquinone A is a selective inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. This compound demonstrates significant biological activity by inhibiting V-abl protein tyrosine kinase with an IC50 value of 0.59 μM. It is utilized in research for investigating EGFR-related signaling pathways and potential therapeutic applications in cancer treatment.
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Paeciloquinone B is an inhibitor of the EGFR (epidermal growth factor receptor) protein tyrosine kinase. This compound demonstrates significant biological activity in obstructing EGFR signaling pathways, making it a valuable tool in cancer research, particularly for the study of tumor growth and proliferation. Its application in the investigation of specific cancer types associated with EGFR overexpression provides insights into potential therapeutic strategies.
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