EGFR/HER2

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.

Cat. No.

A28668

CAS No.

2451398-65-3

TAS2940

TAS2940 is a selective, irreversible pan-ERBB inhibitor that effectively penetrates the blood-brain barrier. It exhibits significant 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 applicable for research focused on tumors exhibiting HER2 and EGFR aberrations, providing valuable insights into targeted cancer therapies.

Cat. No.

A28669

CAS No.

3062177-59-4

EGFR-IN-177

EGFR-IN-177 is a highly selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.32 nM against the EGFR L858R mutation and 0.67 nM against EGFR D746-750, among others. This compound effectively inhibits lung cancer cell proliferation and the phosphorylation of EGFR, demonstrating significant potential for therapeutic applications in non-small cell lung cancer research. EGFR-IN-177 is a valuable tool for exploring mechanisms of resistance and sensitivity in targeted cancer therapies.

Cat. No.

A28670

CAS No.

2890621-88-0

EGFR-IN-126

EGFR-IN-126 is a potent inhibitor targeting the EGFRL858R/T790M/C797S mutations, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant antitumor activity in both in vivo and in vitro models, making it a valuable tool for cancer research and therapeutic development focusing on EGFR-related malignancies.

Cat. No.

A28671

CAS No.

1879071-89-2

EGFR/HER2-IN-4

EGFR/HER2-IN-4 is an irreversible dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits potent inhibition of EGFR with an IC50 of 0.6 nM and effectively inhibits kinase activity associated with L858R and T790M mutations. Demonstrating significant antitumor efficacy in vivo, EGFR/HER2-IN-4 is a valuable reagent for research on lung cancer and related therapeutic strategies.

Cat. No.

A28672

CAS No.

3105969-17-0

EGFR-IN-203

EGFR-IN-203 is a selective inhibitor of the EGFR kinase domain, specifically targeting the mutant forms EGFRT790M, C797S, and V948R. It exhibits a stable binding affinity to the allosteric pocket of EGFR in its inactive conformation. This compound is valuable for research applications focused on cancer, particularly non-small cell lung cancer, providing insights into EGFR-related pathways and potential therapeutic strategies.

Cat. No.

A28673

CAS No.

3032760-70-3

EGFR T790M/L858R-IN-5

EGFR T790M/L858R-IN-5 is a selective inhibitor targeting the EGFR T790M and L858R mutations. It demonstrates a high inhibition percentage of 92.9% at a concentration of 0.05 μM, making it a valuable tool for research into targeted cancer therapies. This compound is primarily utilized in studies aimed at understanding resistance mechanisms in non-small cell lung cancer and the development of effective treatment strategies.

Cat. No.

A28674

CAS No.

3031307-73-7

EGFR-IN-42

EGFR-IN-42 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating single-digit nanomolar activity. This compound forms a covalent linkage between tamoxifen or endoxifen and the EGFR inhibitor gefitinib, allowing it to retain both estrogen receptor antagonist and EGFR inhibitory properties. EGFR-IN-42 shows enhanced anti-cancer activity, making it a valuable tool for research into dual-target therapeutic strategies in cancer treatment.

Cat. No.

A28675

CAS No.

2130982-18-0

ODS-2004436

ODS-2004436 is a small molecule radiotracer that targets the epidermal growth factor receptor (EGFR) for use in positron emission tomography (PET) imaging. This compound exhibits significantly higher uptake in xenograft models of lung cancer harboring EGFR mutations compared to wild-type models, enabling effective differentiation of mutation status. ODS-2004436 is valuable for identifying EGFR-positive tumors and predicting therapeutic responses, particularly in non-small cell lung cancer (NSCLC) research applications.

Cat. No.

A28676

CAS No.

2416925-03-4

EGFR-IN-68

EGFR-IN-68 is a selective inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.33 μM. This compound demonstrates significant anticancer activity, making it valuable for research on tumor proliferation and metastasis. It is particularly useful in studies examining EGFR signaling pathways and developing targeted therapeutic strategies in cancer biology.

Cat. No.

A28677

CAS No.

1262034-38-7

Dacomitinib metabolite M1/2

Dacomitinib metabolite M1/2 is a potent inhibitor of epidermal growth factor receptor (EGFR), effective against both wild-type EGFR and the T790M mutation. This compound shows significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC), making it an important tool for researchers studying cancer treatment and resistance pathways. Its role in targeting resistant NSCLC underscores its relevance in the development of therapeutic strategies.

Cat. No.

A28678

CAS No.

2057423-46-6

EGFR-IN-55

EGFR-IN-55 is a selective inhibitor of the Epidermal Growth Factor Receptor (EGFR), exhibiting potent activities with IC50 values of 70 nM for wild-type EGFR and 3.9 nM for the EGFRL858R/T790M mutant. This compound effectively induces cell cycle arrest in the G0/G1 phase in NCI-H1975 cells, demonstrating significant anticancer activity. EGFR-IN-55 is a valuable tool for research in cancer biology, particularly in studies targeting EGFR-related pathways.

Cat. No.

A28681

CAS No.

118409-58-8

Tyrphostin 25

Synonyms: AG82; Tyrphostin A 25; Tyrphostin AG 82; RG-50875

Tyrphostin 25 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, demonstrating an IC50 of 3 µM in A431 cells. Additionally, this compound acts as an agonist for GPR35, exhibiting an EC50 of 5.3 µM. Tyrphostin 25 is utilized in research applications focused on cancer biology and signal transduction pathways, making it a valuable tool for understanding EGFR-related mechanisms and GPR35 function.

Cat. No.

A28682

CAS No.

137515-05-0

RG-14467

RG-14467 is a selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exerting its action by inhibiting enzymatic activity. It exhibits inhibition kinetics comparable to Lavendustin-A, with a dissociation constant of 3.4 μM for the rapidly formed initial complex and an overall dissociation constant estimated at 30 nM or less. RG-14467 functions as a partially competitive inhibitor of ATP, making it a valuable tool for research applications focused on EGFR-related signaling pathways and cancer therapeutics.

Cat. No.

A28683

CAS No.

1031620-09-3

EGFR/HER2-IN-3

EGFR/HER2-IN-3 is a potent dual inhibitor targeting epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits significant biological activity in inhibiting cell proliferation and tumor growth associated with EGFR and HER2 overexpression. This compound is particularly useful in cancer research, facilitating studies on therapeutic interventions for tumors driven by these pathways.

Cat. No.

A28684

CAS No.

2711105-48-3

EGFR-IN-39

EGFR-IN-39 is a potent inhibitor of the epidermal growth factor receptor (EGFR), a pivotal target in the regulation of cell proliferation. This acrylamide derivative exhibits significant anti-tumor activity with minimal associated toxicity, making it a valuable candidate for cancer research, particularly concerning non-small cell lung cancer (NSCLC). Given its ability to address conditions linked to EGFR overexpression and mutations, EGFR-IN-39 holds promise for advancing the understanding and treatment of EGFR-driven malignancies.

Cat. No.

A28685

CAS No.

2682200-93-5

EGFR-IN-29

EGFR-IN-29 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR). This compound demonstrates significant biological activity in blocking EGFR signaling pathways, which are critical in various tumorigenic processes. EGFR-IN-29 is useful in research applications focused on cancer biology and therapeutic resistance, providing insights into targeted therapy for EGFR-driven malignancies.

Cat. No.

A28686

CAS No.

2660252-31-1

EGFR-IN-114

EGFR-IN-114 is a selective non-covalent inhibitor targeting mutant forms of the epidermal growth factor receptor (EGFR). Demonstrating potent inhibitory activity, it is primarily utilized in research focused on non-small cell lung cancer (NSCLC). This compound provides a valuable tool for studying EGFR signaling pathways and developing targeted therapies in oncological research.

Cat. No.

A28687

CAS No.

2809982-26-9

EGFR-IN-133

EGFR-IN-133 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively targeting various mutations including wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with IC50 values of 0.1, 0.044, 0.036, 0.04, and 0.054 nM, respectively. This compound demonstrates favorable pharmacokinetic properties and exhibits high oral bioavailability, making it a useful tool in molecular biology and cancer research for studying EGFR signaling pathways and developing targeted therapies for EGFR-mutant cancers.

Cat. No.

A28688

CAS No.

2711105-53-0

EGFR-IN-37

EGFR-IN-37 is a selective inhibitor of epidermal growth factor receptor (EGFR), designed to target and disrupt its activity. This compound exhibits significant anti-tumor effects while minimizing toxic side effects, making it suitable for therapeutic research. Given the role of EGFR overexpression and mutations in driving uncontrolled cell proliferation, particularly in non-small cell lung cancer (NSCLC), EGFR-IN-37 presents a valuable tool for investigating EGFR-related malignancies. Its applications extend to the study of disease mechanisms and potential treatment strategies for conditions associated with EGFR mutations.

Cat. No.

A28689

CAS No.

3102899-89-5

EGFR-IN-200

EGFR-IN-200 is a selective inhibitor of the epidermal growth factor receptor (EGFR), with IC50 values of 0.03 μM for EGFR, 3.1 μM for TNF-α, and 1.6 μM for the IL-6/GP130 complex. By binding to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, it induces G2/M cell cycle arrest, apoptosis, and demonstrates potent antiproliferative activity. With high gastrointestinal absorption and low blood-brain barrier permeability, EGFR-IN-200 is valuable for investigating mechanisms in lung cancer and breast adenocarcinoma research.

Cat. No.

A28690

CAS No.

3061531-76-5

EGFR-IN-110

EGFR-IN-110 is a covalent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting pIC50 values of 9.2 for the EGFR enzyme and 8.7 for EGFR-expressing cells. This compound demonstrates robust inhibitory activity against EGFR, coupled with favorable selectivity for kinases. It serves as a valuable tool in research focused on targeting EGFR-related pathways and exploring therapeutic interventions in EGFR-driven cancers.

Cat. No.

A28691

CAS No.

3061364-63-1

EGFR-IN-157

EGFR-IN-157 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 18.81 nM. This compound is primarily utilized in research focused on non-small cell lung cancer (NSCLC), enabling investigations into EGFR-mediated signaling pathways and therapeutic strategies. Its efficacy in inhibiting EGFR activity makes it a valuable tool for studying the molecular mechanisms underlying NSCLC and developing targeted cancer therapies.