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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.
HER2-IN-12 is a potent HER2 inhibitor with an IC50 value of 121 nM. It selectively targets the HER2 receptor, making it a valuable tool in cancer research, particularly in the study and treatment of breast cancer. Its efficacy in inhibiting HER2 activity supports investigations into therapeutic strategies for HER2-positive malignancies.
PKI-166 hydrochloride is a selective and potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 value of 0.7 nM. This compound is primarily utilized in cancer research, particularly in studies focused on EGFR-driven tumors. Its effectiveness in inhibiting EGFR activity makes it a valuable tool for investigating targeted therapies and understanding signaling pathways in oncogenesis.
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.
Synonyms: TRX-13
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-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-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.
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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.
CHNQD-01281 is an EGFR modulator that exhibits potent antiproliferative activity against cancer cells, with IC50 values of 0.079 and 0.081 μM for T24 and J82 cell lines, respectively. This compound effectively regulates both the EGFR/PI3K/AKT and EGFR/ERK signaling pathways, enhancing the chemotactic response of immune effector cells to chemokines. In vivo studies demonstrate that CHNQD-01281 significantly inhibits tumor growth in T24 xenograft mouse models and extends survival in MB49 allogeneic mouse models by promoting the infiltration of cytotoxic T cells.
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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.
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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
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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.
HER2-IN-8 is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2). This compound exhibits significant anti-cancer activity, making it a valuable tool for studying malignancies that overexpress HER2. Additionally, HER2-IN-8 can be utilized in inflammation research, providing insights into its role in related pathological conditions.
LARLLT is an EGFR-binding peptide that specifically targets the epidermal growth factor receptor (EGFR). This compound exhibits potential in the research of cancers characterized by EGFR overexpression, including lung, ovarian, and colorectal cancers. Its application in studies may facilitate insights into tumor biology and therapeutic interventions in EGFR-driven malignancies.
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EGFR-IN-63 is a potent inhibitor of the epidermal growth factor receptor (EGFR), with an IC50 value of 0.096 μM. This compound demonstrates significant anticancer activity, particularly in MCF-7 breast cancer cells, exhibiting an IC50 of 2.49 μM. EGFR-IN-63 is suitable for research applications involving cancer biology and targeted therapies.
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-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.
Synonyms: CP-358774-d6 hydrochloride; NSC 718781-d6 hydrochloride; OSI-774-d6 hydrochloride
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.
AG 1406 is a potent HER2 inhibitor, exhibiting an IC50 of 10.57 μM against the HER2 receptor in BT474 cells, while demonstrating minimal activity against EGFR with an IC50 greater than 50 μM in EGF-3T3 cells. This compound serves as a valuable tool for research focused on HER2-positive cancer models and therapeutic strategies targeting HER2 pathways. AG 1406 is suitable for studies investigating the role of HER2 in tumor progression and resistance mechanisms.
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-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.
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-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-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.
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-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.
