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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR T790M/L858R Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2/CDK9/COX-2 Inhibitor
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. -
EGFR/HER2/DHFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2/CDK9 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2/CDK9 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
JGK-068S is a potent EGFR inhibitor that specifically targets the epidermal growth factor receptor. This compound demonstrates significant biological activity by effectively blocking the signaling pathways associated with tumor growth and proliferation. JGK-068S is commonly utilized in cancer research to investigate its therapeutic potential and mechanisms of action in EGFR-driven malignancies. -
EGFRL858R/T790M Inhibitor
EGFR T790M/L858R-IN-4 is a targeted inhibitor specifically designed to block the mutated forms of the epidermal growth factor receptor (EGFR) associated with non-small cell lung cancer (NSCLC), namely L858R and T790M mutations. This compound exhibits significant anticancer activity, making it a valuable tool for research on targeted therapies and resistance mechanisms in cancer treatment. It is particularly useful in studying drug resistance and evaluating potential therapeutic strategies in EGFR-driven tumor models. -
EGFR Inhibitor
EGFR-IN-189 is a selective covalent inhibitor of the epidermal growth factor receptor (EGFR), with an IC50 value of 200 nM. This compound effectively targets the C797S mutant form of EGFR, demonstrating potent inhibition of cancer cell proliferation. Furthermore, EGFR-IN-189 disrupts EGFR phosphorylation and subsequently inhibits ERK1/2 phosphorylation, making it a valuable tool for research applications in non-small cell lung cancer. -
EGFR Inhibitor
EGFR-IN-33 is a selective inhibitor of the epidermal growth factor receptor (EGFR), designed to target aberrant signaling pathways associated with tumor growth. This acrylamide derivative exhibits significant anti-tumor activity while maintaining low toxicity profiles. EGFR-IN-33 is particularly relevant for research focusing on cancers driven by EGFR mutations and overexpression, including non-small cell lung cancer (NSCLC). Its potential utility in elucidating the mechanisms of EGFR-related malignancies establishes it as a valuable tool in cancer research. -
EGFR Inhibitor
EGFR-IN-49 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 65.0 nM for EGFRT790M and 13.6 nM for EGFRT790M/L858R variants. This compound effectively induces late apoptosis in a dose-dependent manner, making it a valuable tool for studying cancer cell signaling and apoptosis mechanisms. Its potency and selectivity position EGFR-IN-49 as a promising reagent for research applications focused on targeting EGFR-related pathways in cancer therapeutics. -
EGFR Kinase Inhibitor
EGFR-IN-112 is a potent inhibitor of the EGFR kinase, exhibiting IC50 values of 2.31 ± 0.3 μM in MCF-7, 3.16 ± 0.8 μM in H69AR, and 4.2 ± 0.2 μM in PC-3 cancer cell lines. This compound shows selective cytotoxicity towards cancer cells, making it a valuable tool for research in targeted cancer therapies and investigations into EGFR-related signaling pathways. Its efficacy highlights its potential in the study of cancer resistance mechanisms and the development of novel anticancer treatments. -
EGFR Inhibitor
BIEGi-1 is a selective inhibitor of the epidermal growth factor receptor (EGFR), primarily targeting the inhibition of EGFR-Rheb interactions within cells. It significantly suppresses EGFR kinase activity, as evidenced by reduced levels of p-Y1068-EGFR, and also impedes mTORC1 activation by lowering p-T389-S6K1 levels in EGFR-mutant cell lines. BIEGi-1 demonstrates pronounced antiproliferative effects on EGFR-mutant PC9 and HCC827 cells, exhibiting IC50 values of 17 nM and 20 nM, respectively. This compound is a valuable tool for investigating cancers associated with EGFR mutations, notably non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR-IN-199 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 1.1 nM and 1.4 nM for purified EGFR wild-type and EGFRT790M/L858R kinases, respectively. This compound is valuable for cancer research, particularly in studies focused on EGFR signaling pathways and resistance mechanisms in tumor biology. -
EGFR Del19 Inhibitor
EGFR-IN-73 is a selective inhibitor targeting the EGFR Del19 mutation, demonstrating an IC50 value of 119 nM. This compound exhibits potent inhibition of tumor proliferation driven by the prevalent EGFR Del19 mutation. It is suitable for research applications focusing on cancer biology and therapeutic development for EGFR-driven malignancies. -
EGFR Inhibitor
NS-062 is an orally active, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant antiproliferative activity in drug-resistant double mutated H1975 cells, with an IC50 value of 0.19 μM. Furthermore, NS-062 shows antitumor efficacy in an H1975 mouse xenograft model, making it a valuable tool for research on EGFR-related cancer treatments.
