EGFR/HER2

Cat. No.

A25757

CAS No.

1398312-64-5

Afatinib oxalate

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.

Cat. No.

A25773

CAS No.

2411549-88-5

Lazertinib mesylate hydrate

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.

Cat. No.

A25805

CAS No.

2549192-10-9

EGFR-IN-113

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.

Cat. No.

A25849

CAS No.

2769715-68-4

BI-4732

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).

Cat. No.

A25916

CAS No.

2311901-93-4

BAY 2476568

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.

Cat. No.

A25921

CAS No.

2247995-37-3

Lazertinib mesylate

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.

Cat. No.

A25988

CAS No.

6906-38-3

Delphinidin 3-glucoside chloride

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.

Cat. No.

A26002

CAS No.

930856-19-2

ERBB agonist-1

ERBB Agonist-1 is a selective agonist for the ERBB4 receptor, facilitating its dimerization and activating the associated signaling pathway with an EC50 of 10.5 μM. This compound promotes the phosphorylation of key signaling proteins, Akt and ERK1/2, while reducing collagen expression in cardiac fibroblasts. Additionally, ERBB Agonist-1 has demonstrated protective effects against H2O2-induced cardiomyocyte death and Ang II-induced hypertrophy, making it a valuable tool for researching cardiac fibrosis and cardioprotective mechanisms in preclinical models.

Cat. No.

A26879

CAS No.

3038386-42-1

TrxR/EGFR-IN-1

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.

Cat. No.

A26909

CAS No.

1187538-35-7

Lapatinib tosylate

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.

Cat. No.

A28495

CAS No.

2134096-06-1

Almonertinib mesylate

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.

Cat. No.

A28549

CAS No.

2765525-82-2

STX-721

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.

Cat. No.

A28550

CAS No.

1429755-56-5

Tucatinib hemiethanolate

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.

Cat. No.

A28551

CAS No.

1835667-63-4

Befotertinib

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.

Cat. No.

A28552

CAS No.

241127-79-7

NSC689857

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.

Cat. No.

A28553

CAS No.

2890261-81-9

EGFR-IN-61

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.

Cat. No.

A28554

CAS No.

3034701-54-4

EGFR/HER2-IN-14

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.

Cat. No.

A28556

CAS No.

2809982-20-3

EGFR-IN-132

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.

Cat. No.

A28557

CAS No.

2820126-32-5

EGFR/HER2-IN-8

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.

Cat. No.

A28558

CAS No.

1854985-74-2

Lifirafenib maleate

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.

Cat. No.

A28559

CAS No.

2055746-08-0

EGFR-IN-159

EGFR-IN-159 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 29.00 nM. This dihydropyrimidine compound demonstrates dose-dependent inhibition of both EGFR and HER2, leading to significant cytotoxic effects in MCF-7 breast cancer cells and Vero cells, with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. Additionally, EGFR-IN-159 does not cross the blood-brain barrier, making it a valuable candidate for targeted anti-cancer therapies. Its potent anti-cancer activity highlights its potential for research applications in oncology.

Cat. No.

A28561

CAS No.

333419-97-9

EGFR T790M/L858R-IN-8

EGFR T790M/L858R-IN-8 is a selective inhibitor of the epidermal growth factor receptor (EGFR) mutations T790M and L858R, exhibiting an IC50 value of 56.8 μM. This compound is relevant in cancer research, particularly for investigating the effects of these mutations on cell proliferation in various cancer cell lines, including A549, A431, and NHI-H1975. Although the anti-proliferative activity of EGFR T790M/L858R-IN-8 is not significant in these lines, it serves as a useful tool for studying resistance mechanisms in EGFR-targeted therapies.

Cat. No.

A28562

CAS No.

2758904-45-7

EGFR-IN-104

EGFR-IN-104 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.33 μM against the EGFRL858R/T790M mutant and 0.133 μM against the EGFRDel19/T790M/C797S variant. This compound exhibits significant anticancer activity, making it a valuable tool for cancer research and therapeutic studies, particularly in the context of resistant EGFR mutant forms. Its ability to inhibit EGFR signaling pathways positions EGFR-IN-104 as an important reagent for exploring targeted cancer therapies.

Cat. No.

A28563

CAS No.

2230825-46-2

EGFR ligand-14-PEG3-Boc

EGFR ligand-14-PEG3-Boc is a compound designed for targeted conjugation involving the epidermal growth factor receptor (EGFR). This reagent incorporates an EGFR ligand and a polyethylene glycol (PEG) linker, facilitating the synthesis of SJF-1521. It is particularly useful in research applications focusing on drug delivery systems and targeted therapies that exploit the EGFR signaling pathway.

Cat. No.

A28564

CAS No.

1180924-34-8

EGFR/HER2/CDK9-IN-2

EGFR/HER2/CDK9-IN-2 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 145.35 nM, 129.07 nM, and 117.13 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to concurrently inhibit these kinases positions it as a promising candidate for studies focused on targeted therapy and oncogenic signaling pathways.