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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR L858R/T790M Inhibitor
Antiproliferative agent-34 is a selective inhibitor targeting EGFR L858R/T790M with an IC50 of 177 nM, while exhibiting inhibition of EGFR WT at 1567 nM. This compound also effectively inhibits several kinases, including JAK2, ROS1, FLT3, FLT4, and PDGFRα with IC50 values ranging from approximately 30 nM to 226 nM. Antiproliferative agent-34 demonstrates significant anti-proliferative activity in H1975 and HCC827 cancer cell lines, with IC50 values below 40 nM under normoxic conditions, and enhanced potency of 4–6-fold under hypoxic conditions, making it a valuable tool for cancer research focused on targeted therapies. -
EGFR Inhibitor
BPIQ-II hydrochloride is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 value of 8 pM. This compound selectively targets EGFR while showing minimal interaction with various other tyrosine and serine/threonine kinases. In cellular studies, BPIQ-II effectively penetrates cells and specifically disrupts EGF-stimulated signal transduction by competitively binding to the ATP site of EGFR. This makes it a valuable tool for research into EGFR-related signaling pathways and targeted cancer therapies. -
EGFR inhibitor
EGFR-IN-82 is a highly selective and orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.09 nM for the EGFRL858R/T790M/C797S mutant and 0.06 nM for EGFRDel19/T790M/C797S. This compound demonstrates significant anti-proliferative effects and inhibits tumor formation in nude mice models. EGFR-IN-82 is a valuable tool for research into non-small cell lung cancer, particularly in studies focused on resistant EGFR mutations. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-19 is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). This compound exhibits significant anti-proliferative activity in cancer cells driven by EGFR and HER2 signaling pathways. It serves as a valuable tool for research applications focused on understanding and targeting EGFR/HER2-mediated tumorigenesis. -
EGFR Inhibitor
Antiproliferative agent-54 is a potent EGFR inhibitor that targets multiple kinases, including ABL WT, B-RAF, HCK, LYN A, and SRC, with IC50 values ranging from 6 to 50 nM. This compound effectively reduces the proliferation of various cancer cell lines and shows significant inhibitory effects on human umbilical vein endothelial cells (HUVEC) and HepG2 cells, with EC50 values of 34 and 38 nM, respectively. Antiproliferative agent-54 also demonstrates favorable pharmacokinetic properties in rat models, supporting its potential for further research applications in cancer therapy. -
EGFR Inhibitor
EGFR-IN-18 is a selective inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting the L858R/T790M/C797S mutant variant with a potency of 4.9 nM. In contrast, it exhibits reduced activity against wild-type EGFR at 47 nM. This compound is valuable for studying EGFR-driven cancer models and may facilitate the development of targeted therapies in oncology research. -
EGFR Inhibitor
Tyrphostin 8 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 560 μM. Additionally, it acts as a GTPase inhibitor and can effectively inhibit the protein serine/threonine phosphatase calcineurin, with an IC50 of 21 μM. Tyrphostin 8 is utilized in research applications focusing on cancer biology, signal transduction pathways, and the regulation of cellular processes influenced by EGFR signaling. -
EGFR Inhibitor
EGFR-IN-48 is a highly potent and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.193 nM, 0.251 nM, and 10.4 nM against EGFR del19/TM/CS, EGFRLR/TM/CS, and EGFR wild-type, respectively. This compound effectively inhibits the proliferation of BaF3 cells harboring the EGFR del19/T790M/C797S mutation, as well as PC-9 cells with IC50s of 1.526 nM and 66.7 nM, respectively. EGFR-IN-48 is a valuable tool for research focused on cancer therapeutics, particularly in studies regarding EGFR mutation-related resistance mechanisms. -
EGFR Inhibitor
EGFR-IN-198 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting subnanomolar irreversible inhibition. This compound covalently binds to the kinase domain of EGFR, effectively disrupting its autophosphorylation and downstream signaling pathways. EGFR-IN-198 is utilized in research focusing on cancer biology, particularly in studies investigating EGFR-driven tumors and potential therapeutic interventions targeting this pathway. -
EGFR Inhibitor
EGFR-IN-53 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 8.264 µM. This compound demonstrates significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. EGFR-IN-53 can be employed in studies investigating EGFR-mediated signaling pathways, therapeutic resistance, and potential combination therapies in oncology. -
EGFR Inhibitor
EGFR-IN-90 is a potent orally active inhibitor targeting the epidermal growth factor receptor (EGFR). It demonstrates significant inhibitory activity against the EGFRL858R/T790M/C797S mutations, with an IC50 of 5.1 nM. Additionally, EGFR-IN-90 effectively reduces proliferation in the H1975-TM cell line associated with these mutations, exhibiting an IC50 of 0.05 μM. In vivo, it has been shown to inhibit tumor growth in the H1975-TM xenograft tumor model, making it a valuable tool for cancer research focused on EGFR-related pathways. -
EGFR Inhibitor
EGFR-IN-91 is a selective inhibitor of the epidermal growth factor receptor (EGFR), effective against the EGFR L858R/C797S and EGFR exon 19 deletion/C797S mutants. This compound demonstrates significant anticancer activity by inducing tumor regression in patient-derived xenograft models, making it a valuable tool for research in localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutations. Additionally, EGFR-IN-91's ability to penetrate the blood-brain barrier suggests potential applications in treating brain metastases associated with NSCLC. -
EGFR Inhibitor
RG 14921 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound functions as a noncompetitive inhibitor, effectively blocking EGFR signaling pathways and CAMP-dependent kinase activity. RG 14921 is utilized in research applications focused on cancer biology, particularly in studies investigating the role of EGFR in tumorigenesis and therapeutic resistance. -
EGFR Tyrosine Kinase Inhibitor
Simotinib hydrochloride is a selective EGFR tyrosine kinase inhibitor, demonstrating an IC50 of 19.9 nM. This compound exhibits potent antineoplastic activity, making it a valuable tool for cancer research and therapeutic development targeting EGFR-associated malignancies. Its oral bioavailability enhances its potential for in vivo studies. -
EGFR Inhibitor
EGFR-IN-160 is a selective EGFR inhibitor, exhibiting IC50 values of 1.62 μM, 0.49 μM, and 0.98 μM against EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S variants, respectively. This compound effectively induces G2/M and S phase cell cycle arrest and apoptosis in NCI-H522 lung cancer cells, showcasing its potential as an anticancer agent. Additionally, EGFR-IN-160 demonstrates antioxidant properties, as evidenced by its IC50 values of 12.11 µM against DPPH and 8.89 µM against H2O2, further supporting its relevance in cancer research and therapeutic development. -
EGFR Inhibitor
PD 173955 analog 1 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase. This compound demonstrates significant antitumor activity and has been characterized for its toxicological effects. In silico studies have reported an IC50 value of 0.19 μM, indicating its efficacy in modulating EGFR-related signaling pathways, making it a valuable tool for cancer research and therapeutic investigations. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
Mutant EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR L858R/T790 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Tyrosine Kinase Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR/HER2 Inhibitor
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. -
EGFR Inhibitor
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. -
EGFR Inhibitor
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. -
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.
