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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/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.
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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.
Synonyms: SH-1028 mesylate
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-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.
HER2-IN-6 is a potent inhibitor of the HER2 receptor, targeting its kinase activity. This compound demonstrates significant efficacy against both wild-type and mutant forms of HER2, making it valuable for research focused on HER2-mediated tumorigenesis. Additionally, HER2-IN-6 may serve as a useful tool in studies investigating the role of HER2 in various cancer types.
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-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-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.
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.
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HER2-IN-5 is a potent, orally active inhibitor of the HER2 receptor, targeting its role in the proliferation and survival of cancer cells. As a promising agent in cancer research, HER2-IN-5 demonstrates significant anticancer activity by disrupting HER2 signaling pathways. It has potential applications in the development of therapies for HER2-positive cancers, providing a valuable tool for investigating HER2-related mechanisms in oncology.
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-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.
Synonyms: BPI-7711 hydrochloride
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.
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(R)-DZD1516 is the R enantiomer of DZD1516, serving as a potent and selective inhibitor of the HER2 receptor. This compound demonstrates significant inhibition of HER2 signaling pathways, which are often implicated in the progression of various cancers. (R)-DZD1516 is valuable for research applications focused on cancer biology, particularly in studies evaluating therapeutic strategies targeting HER2-positive tumors.
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.
Synonyms: AG30
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.
JNJ28871063 hydrochloride is a highly selective and orally active pan-ErbB kinase inhibitor that targets ErbB1, ErbB2, and ErbB4 with IC50 values of 22 nM, 38 nM, and 21 nM, respectively. This compound effectively inhibits the phosphorylation of critical tyrosine residues in EGFR and ErbB2, disrupting signaling pathways implicated in tumorigenesis. Additionally, JNJ28871063 hydrochloride is capable of crossing the blood-brain barrier and has demonstrated significant antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
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.
Synonyms: ZN-A-1041
Perzebertinib is a potent HER2 inhibitor that demonstrates significant activity in inhibiting BT474 cells with an IC50 of 9.5 nM. Additionally, it targets wild-type EGFR in H838 cells, exhibiting an IC50 of 12 µM. This compound is applicable for research into pathways associated with cancer and inflammation.
Synonyms: HMPL-813
Epitinib is an orally active and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), designed to achieve optimal penetration into the brain. This compound is particularly useful in cancer research due to its ability to inhibit EGFR signaling pathways. Additionally, Epitinib contains an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, which can be harnessed in click chemistry applications for various biological studies.
BI-1622 is a potent and highly selective inhibitor of HER2 (ERBB2), exhibiting an IC50 of 7 nM. This compound demonstrates over 25-fold selectivity against EGFR, making it a valuable tool in targeted cancer therapy. In vivo studies using xenograft mouse models with engineered H2170 and PC9 cells reveal significant antitumor efficacy. Additionally, BI-1622 possesses favorable pharmacokinetic and metabolic properties, supporting its potential for clinical research applications.
SPH5030 is a selective and irreversible inhibitor of the HER2 receptor, targeting both HER2WT and EGFRWT with IC50 values of 3.51 nM and 8.13 nM, respectively. This compound demonstrates significant activity against various HER2 mutant forms, making it a valuable tool in cancer research. SPH5030 is useful for studying HER2-related pathways and developing targeted therapies for HER2-positive cancers.
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-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.
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.
