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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.
Synonyms: BI 1810631
Zongertinib (BI 1810631) is a potent and selective tyrosine kinase inhibitor targeting HER2 and EGFR, with IC50 values of 13 nM and 579 nM, respectively. It exhibits significant antitumor activity and is being investigated for the treatment of multiple solid tumors, particularly those driven by HER2 alterations.
WB-308 is a small molecule EGFR inhibitor, designed to target the epidermal growth factor receptor and its associated signaling pathways. In vitro studies demonstrate that WB-308 effectively reduces the proliferation and clonogenicity of non-small cell lung cancer (NSCLC) cells, leading to G2/M phase arrest and apoptosis. Additionally, it demonstrates tumor growth inhibition in both lung orthotopic transplantation and patient-derived xenograft models. WB-308 was shown to impair the phosphorylation of EGFR, AKT, and ERK1/2 proteins, offering a promising alternative to existing EGFR-targeted therapies with potentially lower cytotoxicity.
Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research.
EGFR-IN-176 is an orally active, ATP-competitive inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), notably the C797S-mediated triple mutant. This compound effectively suppresses AKT signaling pathways and induces apoptosis in Ba/F3 and PC-9 cell lines expressing the EGFR mutations EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S. Selectivity is demonstrated by its lack of inhibition against wild-type EGFR-expressing A431 cells. Additionally, EGFR-IN-176 inhibits ALK enzymatic activity with an IC50 of less than 0.5 nM and serves as a valuable tool for research in non-small cell lung cancer (NSCLC).
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KU004 is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting significant anticancer properties. This quinazoline derivative effectively inhibits the proliferation of human breast cancer SKBR3 cells through the induction of G1 phase cell cycle arrest. KU004 interferes with HER2 and EGFR activation, subsequently blocking downstream signaling pathways such as Akt and Erk, and promotes apoptosis primarily via the extrinsic pathway. Its mechanism makes it a valuable tool for cancer research, particularly in studies targeting breast cancer therapy.
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EGFR kinase-IN-8 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating strong inhibitory activity against both triple-mutated EGFR (L858R/T790M/C797S) and double-mutated EGFR (L858R/T790M), with IC50 values of 3.86 nM and 1.23 nM, respectively. This compound effectively suppresses EGFR phosphorylation, leading to inhibition of downstream signaling pathways, including AKT, STAT3, and MAPK. EGFR kinase-IN-8 has shown promising anticancer efficacy, particularly in the treatment of non-small cell lung cancer.
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Synonyms: BIBW 2992 oxalate
Afatinib oxalate is a potent and irreversible dual specificity inhibitor of the ErbB family, specifically targeting EGFR and HER2. With IC50 values of 0.5 nM for EGFR wild-type, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R/T790M, and 14 nM for HER2, it demonstrates strong inhibitory activity. This compound is primarily utilized in research on esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer, making it valuable for studies focused on these malignancies.
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Lazertinib mesylate hydrate is a selective, irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It demonstrates high potency against both activating mutations and the T790M resistance mutation, effectively inhibiting the phosphorylation of EGFR, AKT, and ERK pathways. This compound induces apoptosis and suppresses tumor growth, particularly in non-small cell lung cancer models, making it valuable for research on brain metastases and targeted cancer therapies.
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EGFR-IN-113 is an EGFR kinase inhibitor with an IC50 of 14.79 μM, effectively targeting the EGFR pathway. This compound induces apoptosis and inhibits cell proliferation through the downregulation of Akt and Erk1/2 signaling pathways. EGFR-IN-113 is suitable for research applications focused on EGFR-driven cancers, including lung, pancreatic, and breast carcinoma.
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BI-4732 is a potent, orally active EGFR inhibitor that functions through reversible, ATP-competitive mechanisms. It selectively inhibits the kinase activity of mutant EGFR variants, including L858R, T790M, and C797S, with IC50 values of 1 nM, while sparing the wild-type EGFR. Furthermore, BI-4732 effectively reduces the phosphorylation of key signaling proteins such as AKT, ERK, and S6K. Its robust intracranial anti-tumor efficacy has been demonstrated in the YU-1097 xenograft model that harbors the EGFR_E19del/T790M/C797S mutation, making it a valuable tool for research in non-small cell lung cancer (NSCLC).
BAY 2476568 is a highly selective inhibitor of EGFR targeting exon 20 insertion variants. It demonstrates potent inhibition of the kinase activity of various EGFR exon 20 mutants, including insASV, insSVD, and insNPG, with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 effectively reduces phosphorylation of EGFR (Y1068), ERK1/2, and Akt (S473) in Ba/F3 cells harboring these mutations. This compound is valuable for investigating non-small cell lung cancer (NSCLC) associated with EGFR exon 20 insertion mutations.
Synonyms: YH25448 mesylate; GNS-1480 mesylate
Lazertinib mesylate is a selective, irreversible inhibitor of the EGFR tyrosine kinase, designed for oral administration and capable of penetrating the central nervous system. It demonstrates high efficacy against both activating mutations and the T790M resistance mutation in EGFR. By inhibiting the phosphorylation of EGFR, AKT, and ERK, Lazertinib mesylate induces apoptosis and hampers tumor growth, as evidenced in mouse models of brain metastases. This compound is primarily utilized in research investigating non-small cell lung cancer.
Synonyms: Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride
Delphinidin 3-glucoside chloride is an EGFR inhibitor known for its role in inducing apoptosis in B cell chronic lymphocytic leukaemia (B CLL). It demonstrates phytoestrogen activity by selectively binding to estrogen receptor beta (ERβ) with an IC50 of 9.7 μM and inhibits EGFR with an IC50 of 2.37 µM. Additionally, Delphinidin 3-glucoside chloride exerts antitumor effects through the pAKT/IRF1/HOTAIR pathway and provides protection against oxidative stress, as well as inhibiting platelet activation and endothelial dysfunction. This compound is useful in cancer research and studies related to hormonal regulation.
TrxR/EGFR-IN-1 is a potent inhibitor targeting both Thioredoxin Reductase (TrxR) and Epidermal Growth Factor Receptor (EGFR). This compound demonstrates significant anti-proliferative effects against Gefitinib-sensitive and resistant lung cancer cells, facilitating apoptosis and tumor cell death. TrxR/EGFR-IN-1 promotes GPX4 protein degradation via autophagolysosomal and proteasomal pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it a valuable tool for studying mechanisms underlying Gefitinib-resistant lung cancer.
Synonyms: GW572016 tosylate; GW2016 tosylate
Lapatinib tosylate is a potent inhibitor targeting the ErbB-2 and EGFR tyrosine kinase domains. With IC50 values of 10.2 nM for EGFR and 9.8 nM for ErbB-2, it effectively blocks signaling pathways associated with cell proliferation and survival. This compound is primarily utilized in cancer research and therapeutic studies, particularly for conditions driven by aberrant ErbB signaling.
Synonyms: HS-10296 mesylate
Almonertinib mesylate is an orally available, irreversible third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. It exhibits potent inhibitory activity against T790M, T790M/L858R, and T790M/Del19 variants, with IC50 values of 0.37 nM, 0.29 nM, and 0.21 nM, respectively, while demonstrating reduced efficacy against wild-type EGFR (3.39 nM). This compound is primarily utilized in the study of non-small cell lung cancer for its potential to overcome resistance in patients with specific EGFR mutations.
STX-721 is an orally active, irreversible covalent inhibitor of the EGFR exon 20 insertion (ex20ins) mutants, specifically targeting their unique dynamic protein states. This compound effectively inhibits the kinase activity of ex20ins mutants, such as NPG, ASV, and SVD, leading to a reduction in phosphorylation of EGFR and downstream ERK signaling. In cellular assays, STX-721 suppresses the proliferation of ex20ins-mutant Ba/F3 cells and human non-small cell lung cancer (NSCLC) cell lines. Additionally, it demonstrates tumor regression in patient-derived xenograft models, making it a valuable tool for studying NSCLC with EGFR or HER2 ex20ins mutations.
Synonyms: Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate
Tucatinib hemiethanolate is a selective inhibitor of the HER2 receptor, displaying potent activity with an IC50 of 8 nM. This orally bioavailable compound is primarily utilized in cancer research, particularly in studies focusing on HER2-positive tumors. Tucatinib's mechanism of action contributes to the understanding of targeted therapies in oncology, making it a valuable reagent for investigating therapeutic interventions.
Synonyms: D-0316
Befotertinib is an orally active EGFR tyrosine kinase inhibitor targeting the epidermal growth factor receptor. It exhibits significant antitumor activity by inhibiting the proliferation of tumor cells, making it relevant for research applications in EGFR T790M-positive non-small cell lung cancer (NSCLC). This compound facilitates the investigation of therapeutic strategies for NSCLC and enhances understanding of resistance mechanisms associated with EGFR mutations.
NSC689857 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and the SCF(SKP2) complex, exhibiting an IC50 of 36 μM for Skp2-Cks1. This compound effectively inhibits the ubiquitylation of p27 with an IC50 of 30 μM. NSC689857 demonstrates variable activity across different cancer types, showing particularly enhanced efficacy against leukemia cell lines, making it a valuable tool for cancer research focusing on EGFR-related pathways and cell cycle regulation.
EGFR-IN-61 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase, exhibiting IC50 values of 42 nM for the L858R/T790M variant, 137 nM for L858R/T790M/C797S, and 743 nM for the wild type. It demonstrates significant antiproliferative effects against A549 and H1975 cell lines, with IC50 values of 2.14 μM and 1.82 μM, respectively. This compound is useful for investigating EGFR-related signaling pathways and therapeutic interventions in cancer research.
EGFR/HER2-IN-14 is a highly selective inhibitor of mutant forms of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) that exhibit resistance to conventional therapeutic agents. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research focused on tumorigenesis and resistance mechanisms in various cancer types. Its use can facilitate the investigation of targeted therapies in cancer research, particularly in patient-derived models expressing these mutant receptors.
EGFR-IN-132 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively targeting both wild-type and various mutant forms, including L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S, with IC50 values of 1.6 nM and lower. This compound demonstrates favorable pharmacokinetic properties and high oral bioavailability, making it suitable for in vivo studies. EGFR-IN-132 holds significant potential for research applications involving cancer therapy, particularly in models of EGFR-driven malignancies.
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EGFR/HER2-IN-8 is a potent inhibitor of the EGFR and HER2 kinases, as well as dihydrofolate reductase (DHFR), displaying IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. This compound demonstrates significant anticancer activity against multiple cancer cell lines while maintaining a favorable safety profile and selectivity. EGFR/HER2-IN-8 is a valuable tool for investigating therapeutics targeting cancer pathways and can contribute to further understanding of cancer biology.
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Synonyms: BGB-283 maleate
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation.
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