EGFR/HER2

Cat. No.

A28635

CAS No.

503443-98-9

EGFR-IN-166

EGFR-IN-166 is a selective inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates potent anticancer activity, exhibiting IC50 values of 69.63 μM and 22.84 μM against MCF-7 and MDA-MB-231 breast cancer cell lines, respectively. In addition to its cytotoxic effects, EGFR-IN-166 significantly reduces cell migration and decreases EGFR expression. This reagent is valuable for research in breast cancer therapies and mechanisms of EGFR signaling.

Cat. No.

A28636

CAS No.

3077345-85-5

EGFR-IN-202

EGFR-IN-202 is an inhibitor of the epidermal growth factor receptor (EGFR) that specifically targets exon 20 insertion mutations. This compound demonstrates significant biological activity by inhibiting aberrant signaling pathways associated with non-small cell lung cancer (NSCLC). EGFR-IN-202 is suitable for research applications focused on understanding the mechanisms of resistance in NSCLC and evaluating potential therapeutic strategies.

Cat. No.

A28637

CAS No.

133550-22-8

EGFR-IN-16

EGFR-IN-16 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR) with a pIC50 of 4.85. Additionally, it exhibits inhibition of HER-2 with a pIC50 of 4.74, emphasizing its dual-target potential. This compound is useful for research focused on cancer biology, particularly in studies involving EGFR and HER-2 signaling pathways. EGFR-IN-16 can aid in the development of therapeutic strategies for EGFR-driven malignancies.

Cat. No.

A28639

CAS No.

2758034-98-7

TAS2940 fumarate

TAS2940 fumarate is an irreversible and selective pan-ERBB inhibitor that effectively penetrates the blood-brain barrier. It demonstrates potent inhibitory activity against wild-type HER2, HER2 V777L, and A775_G776insYVMA, with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. This compound is suitable for research applications focused on tumors characterized by HER2 and EGFR mutations.

Cat. No.

A28641

CAS No.

3034701-46-4

EGFR/HER2-IN-13

EGFR/HER2-IN-13 is a potent inhibitor targeting mutant forms of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) that exhibit resistance to conventional therapies. This compound demonstrates significant biological activity against these mutants, making it a valuable tool for cancer research, particularly in studies aimed at understanding resistance mechanisms and developing novel therapeutic strategies.

Cat. No.

A28642

CAS No.

1135150-79-6

EGFR/ErbB-2 inhibitor-1

EGFR/ErbB-2 inhibitor-1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR) and ErbB-2/HER2. This compound demonstrates potent inhibition of EGFR-related signaling pathways and is used in research focused on cancer therapies, particularly breast cancer and other tumors overexpressing HER2. Its ability to interfere with receptor dimerization and downstream signaling makes it valuable for studies on targeted cancer treatments and resistance mechanisms.

Cat. No.

A28643

CAS No.

2412155-75-8

AST5902 mesylate

AST5902 mesylate is a potent EGFR inhibitor that demonstrates significant antineoplastic activity. As a principal metabolite of Alflutinib, it plays a crucial role in the treatment of non-small cell lung cancer, effectively targeting activating EGFR mutations. Additionally, AST5902 mesylate shows promise in overcoming resistance associated with the EGFR T790M mutation, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A28646

CAS No.

3031307-74-8

EGFR-IN-43

EGFR-IN-43 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with sub-nanomolar activity. This compound uniquely fuses tamoxifen or endoxifen with the EGFR inhibitor gefitinib through a covalent bond, allowing it to exhibit both estrogen receptor antagonist properties and effective EGFR inhibition. EGFR-IN-43 demonstrates enhanced anti-cancer effects, making it a valuable tool for studies on targeted therapies in cancer research.

Cat. No.

A28647

CAS No.

2543763-00-2

EGFR-IN-123

EGFR-IN-123 is a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates significant efficacy against cancer cell lines, including PC-9G, A549, A431, and HCT116, with IC50 values of 0.74, 1.36, 1.20, and 2.53 μM, respectively. EGFR-IN-123 is suitable for research applications focused on targeted cancer therapies and understanding EGFR signaling pathways.

Cat. No.

A28648

CAS No.

122520-86-9

Tyrphostin AG213

Synonyms: AG213

Tyrphostin AG213 is a selective inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.85 μM, targeting its protein tyrosine kinase activity. In addition to its primary function, Tyrphostin AG213 also inhibits tyrosine kinase activity with an IC50 of 2.4 μM and topoisomerase II, exhibiting an IC100 of 50 μM. This compound has been shown to induce non-apoptotic programmed cell death in tumor cells, making it a valuable tool for cancer research and potential therapeutic applications.

Cat. No.

A28649

CAS No.

2416924-99-5

EGFR-IN-67

EGFR-IN-67 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 0.34 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and targeted therapeutic strategies against EGFR-overexpressing tumors. Researchers can utilize EGFR-IN-67 to investigate the role of EGFR signaling in various cancer types and explore potential treatment modalities.

Cat. No.

A28650

CAS No.

360760-58-3

EG31

EG31 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting strong antiproliferative effects on triple-negative breast cancer (TNBC) cells, with GI50 values of 498.90 nM for MDA-MB-231 and 740.73 nM for Hs578T cell lines. It effectively induces apoptosis by disrupting the EGFR signaling pathway. Additionally, EG31 retains its efficacy against 5-fluorouracil (5-FU)-resistant TNBC cells, demonstrating a GI50 of 519.5 nM. This compound is valuable for researching mechanisms of resistance in TNBC.

Cat. No.

A28653

CAS No.

3103654-99-2

EGFR-IN-201

EGFR-IN-201 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.091 μM against wild-type EGFR. It demonstrates activity against mutant EGFR variants, with IC50 values of 0.147 μM for EGFRT790M, 0.221 μM for EGFRL858R, and 0.703 μM for EGFRC797S. Inhibition of downstream signaling pathways is evidenced by its IC50 values of 0.225 μg/mL for AKT1 and 0.705 μg/mL for ERK1. EGFR-IN-201 has been shown to induce G0/G1 cell cycle arrest, apoptosis, and low-level necrosis in cancer cells, making it a valuable tool for research in various cancer types, including colon cancer.

Cat. No.

A28654

CAS No.

3032760-90-7

EGFR T790M/L858R-IN-7

EGFR T790M/L858R-IN-7 is a potent inhibitor of the EGFR L858R and T790M mutations, demonstrating a remarkable 93% inhibition rate at a concentration of 0.05 μM. This novel pyrimidine compound operates by selectively targeting the kinase domain of the epidermal growth factor receptor (EGFR), effectively suppressing its phosphorylation activity. It is a valuable tool for research applications focused on understanding resistance mechanisms in non-small cell lung cancer (NSCLC) and developing targeted therapies.

Cat. No.

A28655

CAS No.

2387574-01-6

HER2-IN-7

HER2-IN-7 is a potent inhibitor of the HER2 receptor, which is part of the ErbB family of signaling proteins. This compound effectively interferes with pathways involved in cell proliferation, invasion, angiogenesis, and tumor cell survival. HER2-IN-7 is valuable for research applications targeting HER2-related diseases, particularly various forms of cancer.

Cat. No.

A28656

CAS No.

848439-89-4

AZ5385

AZ5385 is an EGFR-tyrosine kinase inhibitor that effectively modulates signaling pathways involved in cell proliferation and survival. This compound also demonstrates antiviral activity, specifically against HRV-2, with an EC50 value of 0.35 µM, targeting the late stages of the viral life cycle. AZ5385 is applicable in research focusing on cancer therapeutics and virology studies.

Cat. No.

A28657

CAS No.

174709-30-9

BPIQ-I

Synonyms: PD 159121

BPIQ-I is a potent ATP-competitive inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It exhibits significant anti-proliferative activity in various cancer cell lines by interfering with downstream signaling pathways essential for tumor growth and survival. This compound is primarily utilized in cancer research to elucidate the role of EGFR in oncogenic processes and to explore therapeutic strategies targeting EGFR-mediated signaling.

Cat. No.

A28658

CAS No.

2982583-44-6

EGFR-IN-101

EGFR-IN-101 is a selective inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates potent inhibitory activity with IC50 values of 33.26 nM against the EGFRL858R/T790M/C797S mutation and 106.4 nM in Ba/F3-EGFRL858R/T790M/C797S cells. EGFR-IN-101 is valuable for research applications focused on non-small cell lung cancer (NSCLC) and provides a framework for investigating resistance mechanisms and therapeutic strategies targeting EGFR mutations.

Cat. No.

A28660

CAS No.

24909-18-0

NSC114126

NSC114126 is a highly effective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. This compound demonstrates significant antiproliferative activity, making it a valuable tool for cancer research. Its potency and oral bioavailability facilitate the study of EGFR-related pathways in various cancer mechanisms.

Cat. No.

A28661

CAS No.

1454651-67-2

EGFR-IN-180

EGFR-IN-180 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting both wild-type and the drug-resistant L858R/T790M/C797S mutation, with IC50 values of 80.96 nM and 16.43 nM, respectively. This compound serves as an important tool for investigating therapeutic options in non-small cell lung cancer (NSCLC) research, enabling studies on resistance mechanisms and potential combination therapies. Its specific action on EGFR pathways makes it a valuable reagent in cancer biology and pharmacological development.

Cat. No.

A28662

CAS No.

2416924-93-9

EGFR-IN-64

EGFR-IN-64 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating significant potency with an IC50 value of 0.33 μM. This compound has been identified for its potential anticancer activity, making it a valuable tool for research focused on EGFR-related signaling pathways and therapeutic strategies in oncology. Researchers may utilize EGFR-IN-64 to explore the mechanisms of tumor growth and resistance in EGFR-driven cancers.

Cat. No.

A28663

CAS No.

2418549-30-9

EGFR-IN-54

EGFR-IN-54 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 1.623 µM. This compound exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Its inhibitory effects on EGFR can be utilized in studies aimed at understanding cancer proliferation and developing targeted therapies.

Cat. No.

A28664

CAS No.

91769-08-3

EGFR-IN-147

EGFR-IN-147 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an inhibition rate of 14% at a concentration of 1 μM. This compound plays a critical role in cancer research, providing a valuable tool for investigating EGFR-related signaling pathways and therapeutic interventions in various malignancies. Its specificity towards EGFR can aid in studies aimed at understanding tumor growth and resistance mechanisms.

Cat. No.

A28666

CAS No.

1000599-06-3

Tesevatinib tosylate

Synonyms: XL-647 tosylate; EXEL-7647 tosylate; KD-019(tosylate)

Tesevatinib tosylate is a potent inhibitor of the epidermal growth factor receptor (EGFR), capable of penetrating the blood-brain barrier. This compound exhibits significant cytotoxic effects, demonstrating IC50 values of 11 nM and 102 nM against GBM12 and GBM6 cell lines, respectively. Additionally, Tesevatinib tosylate inhibits HER2 (IC50 = 16.1 nM), VEGFR2 (IC50 = 1.5 nM), and Src (IC50 = 10.3 nM), making it a valuable tool for studying tumor proliferation and antitumor activity in various cancer research applications.

Cat. No.

A28667

CAS No.

2444364-04-7

EGFR/HER2/TS-IN-2

EGFR/HER2/TS-IN-2 is a potent inhibitor targeting the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and thymidylate synthase (TS), demonstrating IC50 values of 0.173, 0.125, and 1.12 µM, respectively. This compound exhibits significant cytotoxic activity against MDA-MB-231 breast cancer cell lines, with an IC50 of 1.69 µM. It is a valuable tool for research focused on cancer therapy and the study of tumor biology related to EGFR and HER2 signaling pathways.