EGFR/HER2

Cat. No.

A28692

CAS No.

2472802-77-8

Emupertinib

Emupertinib is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of less than 0.3 nM for the EGFR d746-750/T790M/C779S mutant and up to 0.92 nM for wild-type EGFR. This compound effectively inhibits various EGFR mutations, including L858R/T790M/C797S and d746-750/C797S, making it a valuable tool for research on targeted therapies in cancer treatment. Its high specificity and efficacy position Emupertinib as a significant candidate for studying EGFR-related signaling pathways and developing novel anticancer agents.

Cat. No.

A28693

CAS No.

2634646-14-1

EGFR-IN-22

EGFR-IN-22 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating potent activity with IC50 values of 4.91 nM for wild type EGFR and 0.54 nM for the mutant variants EGFR L858R/T790M/C797S. This compound is valuable for preclinical research aimed at understanding the role of EGFR signaling in various cancers, particularly those harboring specific mutations associated with resistance to standard therapies.

Cat. No.

A28694

CAS No.

2711105-50-7

EGFR-IN-38

EGFR-IN-38 is a selective inhibitor of the epidermal growth factor receptor (EGFR), which plays a critical role in cancer cell proliferation. This compound exhibits significant anti-tumor activity while maintaining low toxicity, making it a valuable tool in cancer research. Its mechanism of action addresses the overexpression and mutations of EGFR, commonly implicated in the development and progression of various malignancies, particularly non-small cell lung cancer (NSCLC). EGFR-IN-38 serves as a promising candidate for investigating EGFR-related pathologies and therapeutic strategies.

Cat. No.

A28696

CAS No.

2820126-28-9

EGFR/HER2-IN-7

EGFR/HER2-IN-7 is a selective inhibitor targeting the EGFR and HER2 kinases, demonstrating potent antitumor activity in MCF-7 breast cancer cells. With IC50 values of 0.18 μM for EGFR and 0.146 μM for HER2, it effectively impedes signaling pathways involved in cancer progression. Additionally, EGFR/HER2-IN-7 exhibits moderate inhibition of dihydrofolate reductase (DHFR) with an IC50 of 0.907 μM. This compound is relevant for research focused on therapeutic strategies for breast cancer and the modulation of related signaling pathways.

Cat. No.

A28701

CAS No.

2968419-65-8

EGFR-IN-81

EGFR-IN-81 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting both wild-type and mutant forms (L858R/T790M) with IC50 values of 4.38 nM and 5.69 nM, respectively. This compound exhibits significant cytotoxic effects on cancer cell lines, demonstrating inhibitory concentrations of 2.07 μM against MCF-7 cells and 6.72 μM against HCT116 cells. EGFR-IN-81 is useful for research applications focused on cancer biology and therapeutic development targeting EGFR-driven malignancies.

Cat. No.

A28703

CAS No.

3000483-29-1

VEGFR-IN-4

VEGFR-IN-4 is a potent epidermal growth factor receptor (EGFR) inhibitor. It demonstrates significant antiproliferative activity, exhibiting an IC50 value of 24.6 nM against HCC827 cells. This compound is primarily utilized in research focused on cancer therapeutics, particularly in studies exploring EGFR-mediated signaling pathways and tumor growth inhibition.

Cat. No.

A28705

CAS No.

2044508-48-5

EGFR-IN-50

EGFR-IN-50 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting the L858R resistance mutation. It exhibits strong anti-proliferative activity in cancer cells, with a GI50 of 8 nM against TEL-EGFR-L858R-BaF3 cells and 6.03 μM against TEL-EGFR-T790M-L858R-BaF3 cells. This compound is valuable for research applications focused on overcoming resistance in EGFR-driven cancers.

Cat. No.

A28707

CAS No.

1033006-96-0

NSC381467

NSC381467 is a potent, orally active inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research. NSC381467 is suitable for studies aimed at understanding EGFR-mediated signaling pathways and their implications in tumor biology.

Cat. No.

A28710

CAS No.

3078678-28-8

EGFR-IN-179

EGFR-IN-179 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 0.068 μM for the EGFR L858R/T790M/C797S mutant and 2.56 μM for wild-type EGFR. This compound exhibits significant anticancer activity, particularly against non-small cell lung cancer, making it a valuable tool for research into targeted therapies and understanding resistance mechanisms in cancer treatment.

Cat. No.

A28711

CAS No.

220576-72-7

EGFR-IN-451

EGFR-IN-451 is a potent EGFR inhibitor, demonstrating an IC50 value of 0.02 nM. This compound effectively targets mutant variants of EGFR, including EGFRL858R, EGFRT790M, and EGFRL858R/T790M, with IC50 values ranging from 0.26 to 34 nM. EGFR-IN-451 significantly inhibits the activation of downstream signaling proteins AKT and ERK, leading to reduced proliferation in EGFR-mutant cancer cell lines. It is suitable for research focused on EGFR-driven malignancies.

Cat. No.

A28712

CAS No.

1223377-83-0

Z118332870

Z118332870 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and bromodomain-containing protein 4 (BRD4). This compound displays significant antitumor activity, making it a promising candidate for addressing resistance mechanisms in cancer therapy. Its dual targeting capability may enhance therapeutic efficacy in various cancer types.

Cat. No.

A28713

CAS No.

1038061-96-9

CDK9-IN-41

CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications.

Cat. No.

A28714

CAS No.

2820126-37-0

EGFR/HER2/DHFR-IN-1

EGFR/HER2/DHFR-IN-1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and dihydrofolate reductase (DHFR). This compound demonstrates potent antitumor efficacy, with IC50 values of 0.153 μM for EGFR, 0.108 μM for HER2, and 0.291 μM for DHFR. EGFR/HER2/DHFR-IN-1 effectively arrests the cell cycle at the G1/S phase and promotes apoptosis in MCF-7 breast cancer cells, making it a valuable reagent for cancer research and therapeutic development.

Cat. No.

A28715

CAS No.

2151881-74-0

SIQ17

SIQ17 is a potent inhibitor of the epidermal growth factor receptor (EGFR) that acts by binding to the ATP-binding site, exhibiting an IC50 of 0.62 nM. This compound demonstrates superior inhibitory activity against EGFR tyrosine kinase compared to Erlotinib, which has an IC50 of approximately 20 nM. SIQ17 is applicable in cancer research, particularly in studies focusing on EGFR-mediated signaling pathways and therapeutic resistance.

Cat. No.

A28716

CAS No.

422276-47-9

EGFR/HER2/CDK9-IN-3

EGFR/HER2/CDK9-IN-3 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 191.08 nM, 132.65 nM, and 113.98 nM, respectively. This compound demonstrates significant antitumor activity, making it valuable for research in cancer therapies and signaling pathways involving these targets. Its inhibitory effects on cell proliferation in cancer models may aid in the understanding and development of targeted treatment strategies.

Cat. No.

A28717

CAS No.

1980848-48-3

HNPMI

HNPMI is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting cytotoxic effects on cancer cells. This compound disrupts the expression of key proteins, including osteopontin, survivin, and cathepsin S, ultimately promoting apoptosis. Additionally, HNPMI influences the BCL-2/BAX ratio and p53 pathways in colorectal cancer cell lines, contributing to the inhibition of tumorigenesis and providing valuable insights for cancer research.

Cat. No.

A28718

CAS No.

2752328-62-2

EGFR-IN-27

EGFR-IN-27 is a highly effective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of less than 50 nM against various mutations, including EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S. This compound is essential for research focused on targeted cancer therapies, particularly in understanding the mechanisms of resistance in non-small cell lung cancer. Its specificity for multiple EGFR mutations makes it a valuable tool for investigating pathways associated with tumor progression and treatment response.

Cat. No.

A28719

CAS No.

879730-44-6

EGFR/HER2/CDK9-IN-1

EGFR/HER2/CDK9-IN-1 is a highly active inhibitor of EGFR, HER2, and CDK9, displaying IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively. This compound demonstrates significant antitumor properties, making it a valuable tool for cancer research. Its ability to target multiple kinases involved in cell proliferation and survival pathways supports investigations into therapeutic strategies for various malignancies.

Cat. No.

A28721

CAS No.

2726463-68-7

EGFR-IN-30

EGFR-IN-30 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values in the range of 1-10 nM and less than 1 nM for both wild-type EGFR and mutant forms (L858R/T790M/C797S). Its strong inhibitory activity positions EGFR-IN-30 as a valuable reagent for investigating cell proliferative diseases, particularly in cancer research applications where modulation of the EGFR signaling pathway is essential.

Cat. No.

A28722

CAS No.

2414056-34-9

HER2-IN-13

HER2-IN-13 is a selective HER2 inhibitor with an IC50 of 8 nM, demonstrating potent inhibition of the HER2 receptor. Additionally, it also inhibits wild-type EGFR with an IC50 of 0.40 μM. This compound is valuable for research applications focused on cancer biology, specifically in studying HER2-driven tumors and EGFR-related pathways.

Cat. No.

A28723

CAS No.

2781912-10-3

EGFR-IN-102

EGFR-IN-102 is a potent inhibitor of the epidermal growth factor receptor (EGFR), displaying an IC50 value of 2 nM. This compound is designed for oral administration and shows significant activity in the study of non-small-cell lung cancer (NSCLC). Its selectivity and efficacy make it a valuable tool for research focused on targeting EGFR-driven tumorigenesis and exploring therapeutic strategies in cancer treatment.

Cat. No.

A28724

CAS No.

2701553-78-6

EGFR-IN-32

EGFR-IN-32 is a potent inhibitor of the epidermal growth factor receptor (EGFR). Activation and dysregulation of EGFR are implicated in the uncontrolled proliferation of cells and the advancement of numerous cancers, particularly non-small cell lung cancer (NSCLC). This compound is valuable for research into diseases driven by EGFR mutations, facilitating investigations into therapeutic interventions targeting this oncogenic pathway.

Cat. No.

A28726

CAS No.

2931499-82-8

EGFR/HER2-IN-10

EGFR/HER2-IN-10 is a selective dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values of 2.3 nM and 234 nM for EGFR and HER2, respectively. This compound demonstrates significant antiproliferative effects against prostate carcinoma, making it a valuable tool for research in cancer biology and targeted therapy development. Its specificity for both EGFR and HER2 positions it as a promising candidate for further investigations into dual receptor inhibition and its therapeutic potential.

Cat. No.

A28728

CAS No.

2642197-17-7

Lunaxafusp

Lunaxafusp is an anti-ERBB2 monoclonal antibody that features a single-chain variable fragment fused to both an antibody heavy chain and a kappa light chain. This reagent exhibits targeted action against the ERBB2 protein, known for its role in various cancers. Lunaxafusp is primarily utilized in research focused on cancer therapeutics and the characterization of ERBB2-related signaling pathways.

Cat. No.

A28729

CAS No.

1196531-39-1

Sapitinib fumarate

Synonyms: AZD-8931 fumarate

Sapitinib fumarate is a reversible, ATP-competitive inhibitor of the ErbB family, specifically targeting EGFR, ErbB2, and ErbB3 with IC50 values of 4 nM, 3 nM, and 4 nM, respectively. This compound exhibits potent inhibition of cellular proliferation driven by aberrant ErbB signaling pathways. It is commonly employed in research focused on cancer biology, particularly in studies investigating therapeutic resistance and receptor tyrosine kinase signaling.