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Catalog No.
Product Name
Application
Product Information
Citations
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ErbB-2/EGFR Inhibitor
Lapatinib ditosylate monohydrate is a selective inhibitor of the ErbB-2 and EGFR tyrosine kinase domains. It demonstrates potent biological activity with IC50 values of 10.2 nM against EGFR and 9.8 nM against ErbB-2. This compound is commonly utilized in cancer research to investigate mechanisms of tumor growth and resistance, particularly in breast cancer models. -
EGFR Inhibitor
T-1-PMPA is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating significant apoptotic effects. This compound effectively targets both wild-type EGFR (EGFRWT) and the EGFR 790M mutation, exhibiting IC50 values of 86 nM and 561.73 nM, respectively. T-1-PMPA is suitable for research applications focused on cancer biology and therapeutic efficacy in EGFR-related pathways. -
EGFR Inhibitor
Khellin is a furochromone that acts as an inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.15 µM. It demonstrates significant anti-proliferative activity in vitro, making it a valuable compound for cancer research. Additionally, Khellin exhibits antispasmodic properties and coronary vasodilator effects, further broadening its potential applications in biological studies. -
EGFR Tyrosine Kinase Inhibitor
Olmutinib hydrochloride is an orally active and irreversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. By covalently binding to a cysteine residue in the kinase domain, it effectively disrupts signaling pathways associated with non-small cell lung cancer (NSCLC). This compound is utilized in research to study the mechanisms of EGFR-related oncogenesis as well as potential therapeutic strategies for NSCLC treatment. -
Mutant-Selective EGFR Inhibitor
Osimertinib mesylate is a mutant-selective inhibitor of the epidermal growth factor receptor (EGFR), acting through a covalent and irreversible mechanism. It demonstrates potent biological activity with an apparent IC50 of 12 nM against the L858R mutation and 1 nM against the L858R/T790M mutation. Osimertinib mesylate is primarily utilized in research focused on overcoming T790M-mediated resistance to existing EGFR-targeted therapies in lung cancer. -
EGFR Inhibitor
Almonertinib mesylate is an orally available, irreversible third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. It exhibits potent inhibitory activity against T790M, T790M/L858R, and T790M/Del19 variants, with IC50 values of 0.37 nM, 0.29 nM, and 0.21 nM, respectively, while demonstrating reduced efficacy against wild-type EGFR (3.39 nM). This compound is primarily utilized in the study of non-small cell lung cancer for its potential to overcome resistance in patients with specific EGFR mutations. -
EGFR Inhibitor
STX-721 is an orally active, irreversible covalent inhibitor of the EGFR exon 20 insertion (ex20ins) mutants, specifically targeting their unique dynamic protein states. This compound effectively inhibits the kinase activity of ex20ins mutants, such as NPG, ASV, and SVD, leading to a reduction in phosphorylation of EGFR and downstream ERK signaling. In cellular assays, STX-721 suppresses the proliferation of ex20ins-mutant Ba/F3 cells and human non-small cell lung cancer (NSCLC) cell lines. Additionally, it demonstrates tumor regression in patient-derived xenograft models, making it a valuable tool for studying NSCLC with EGFR or HER2 ex20ins mutations. -
EGFR Inhibitor
Befotertinib is an orally active EGFR tyrosine kinase inhibitor targeting the epidermal growth factor receptor. It exhibits significant antitumor activity by inhibiting the proliferation of tumor cells, making it relevant for research applications in EGFR T790M-positive non-small cell lung cancer (NSCLC). This compound facilitates the investigation of therapeutic strategies for NSCLC and enhances understanding of resistance mechanisms associated with EGFR mutations. -
EGFR/SKP2 Inhibitor
NSC689857 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and the SCF(SKP2) complex, exhibiting an IC50 of 36 μM for Skp2-Cks1. This compound effectively inhibits the ubiquitylation of p27 with an IC50 of 30 μM. NSC689857 demonstrates variable activity across different cancer types, showing particularly enhanced efficacy against leukemia cell lines, making it a valuable tool for cancer research focusing on EGFR-related pathways and cell cycle regulation. -
EGFR Inhibitor
EGFR-IN-61 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase, exhibiting IC50 values of 42 nM for the L858R/T790M variant, 137 nM for L858R/T790M/C797S, and 743 nM for the wild type. It demonstrates significant antiproliferative effects against A549 and H1975 cell lines, with IC50 values of 2.14 μM and 1.82 μM, respectively. This compound is useful for investigating EGFR-related signaling pathways and therapeutic interventions in cancer research. -
Mutant EGFR/HER2 Inhibitor
EGFR/HER2-IN-14 is a highly selective inhibitor of mutant forms of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) that exhibit resistance to conventional therapeutic agents. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research focused on tumorigenesis and resistance mechanisms in various cancer types. Its use can facilitate the investigation of targeted therapies in cancer research, particularly in patient-derived models expressing these mutant receptors. -
EGFR Inhibitor
EGFR-IN-132 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively targeting both wild-type and various mutant forms, including L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S, with IC50 values of 1.6 nM and lower. This compound demonstrates favorable pharmacokinetic properties and high oral bioavailability, making it suitable for in vivo studies. EGFR-IN-132 holds significant potential for research applications involving cancer therapy, particularly in models of EGFR-driven malignancies. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-8 is a potent inhibitor of the EGFR and HER2 kinases, as well as dihydrofolate reductase (DHFR), displaying IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. This compound demonstrates significant anticancer activity against multiple cancer cell lines while maintaining a favorable safety profile and selectivity. EGFR/HER2-IN-8 is a valuable tool for investigating therapeutics targeting cancer pathways and can contribute to further understanding of cancer biology. -
Raf/EGFR Inhibitor
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation. -
EGFR Inhibitor
EGFR-IN-159 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 29.00 nM. This dihydropyrimidine compound demonstrates dose-dependent inhibition of both EGFR and HER2, leading to significant cytotoxic effects in MCF-7 breast cancer cells and Vero cells, with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. Additionally, EGFR-IN-159 does not cross the blood-brain barrier, making it a valuable candidate for targeted anti-cancer therapies. Its potent anti-cancer activity highlights its potential for research applications in oncology. -
EGFR(T790M/L858R) Inhibitor
EGFR T790M/L858R-IN-8 is a selective inhibitor of the epidermal growth factor receptor (EGFR) mutations T790M and L858R, exhibiting an IC50 value of 56.8 μM. This compound is relevant in cancer research, particularly for investigating the effects of these mutations on cell proliferation in various cancer cell lines, including A549, A431, and NHI-H1975. Although the anti-proliferative activity of EGFR T790M/L858R-IN-8 is not significant in these lines, it serves as a useful tool for studying resistance mechanisms in EGFR-targeted therapies. -
EGFR Inhibitor
EGFR-IN-104 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.33 μM against the EGFRL858R/T790M mutant and 0.133 μM against the EGFRDel19/T790M/C797S variant. This compound exhibits significant anticancer activity, making it a valuable tool for cancer research and therapeutic studies, particularly in the context of resistant EGFR mutant forms. Its ability to inhibit EGFR signaling pathways positions EGFR-IN-104 as an important reagent for exploring targeted cancer therapies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-2 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 145.35 nM, 129.07 nM, and 117.13 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to concurrently inhibit these kinases positions it as a promising candidate for studies focused on targeted therapy and oncogenic signaling pathways. -
EGFR T790M/L858R Inhibitor
EGFR T790M/L858R-IN-6 is a pyrimidine-based inhibitor specifically targeting the EGFR mutations T790M and L858R. This compound demonstrates potent inhibitory activity, achieving 90.88% inhibition of enzyme activity at a concentration of 0.05 μM. It serves as a valuable tool for research focused on the development of targeted therapies for EGFR-mutant cancers. -
EGFR Inhibitor
UNC-CA359 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 value of 18 nM. This compound exhibits significant anti-tumor activity and is particularly applicable in chordoma research. Additionally, UNC-CA359 features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool in click chemistry applications. -
EGFR Inhibitor
EGFR-IN-136 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 20.2 nM for EGFRWT, 1.2 nM for EGFRLR/TM, 2.3 nM for EGFR19D/TM/CS, and 12.5 nM for EGFRLR/TM/CS. This compound exhibits significant antiproliferative and antitumor activity, making it a valuable tool for research involving non-small cell lung cancer (NSCLC). Its selective inhibition of various EGFR mutations positions EGFR-IN-136 as an important reagent for investigating therapeutic strategies targeting EGFR-related pathways. -
EGFR Inhibitor
EGFR-IN-145 is a selective inhibitor of the epidermal growth factor receptor (EGFR) kinase. At a concentration of 20 μM, it demonstrates a 52.7% inhibition of EGFR-wild type kinase activity. This compound is valuable for research in cancer biology, particularly in the study of oncogenic signaling pathways and the development of targeted therapies for EGFR-driven tumors. -
EGFR-TK Inhibitor
NSC81111 is a potent orally active inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK), demonstrating an IC50 of 0.15 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its efficacy in targeting EGFR pathways positions NSC81111 as a promising candidate for studies focused on cancer therapeutics and mechanisms of resistance. -
EGFR Inhibitor
Paeciloquinone D is an inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It exhibits significant biological activity by blocking EGFR signaling pathways, which are critical in tumor growth and proliferation. This compound is relevant for research applications focused on cancer biology and targeted therapies for EGFR-driven malignancies. -
EGFR Tyrosine Kinase Inhibitor
BML-265 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It disrupts Golgi integrity and inhibits the secretory transport of various protein cargos in human cells, but shows no effect in rodent cells. This specificity makes BML-265 a valuable tool for studying EGFR signaling pathways and Golgi function in human cellular contexts. -
EGFR Inhibitor
Tyrphostin 63 is a selective inhibitor of the epidermal growth factor receptor (EGFR). Exhibiting an IC50 value of 375 μM and a Ki value of 123 μM, Tyrphostin 63 effectively modulates EGFR signaling pathways. This compound is primarily utilized in cancer research to investigate the role of EGFR in tumor proliferation and metastasis. -
EGFR Inhibitor
EGFR-IN-149 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.42 nM. This compound effectively blocks EGFR signaling, which is crucial in regulating cellular proliferation and survival. Its prominent biological activity makes it a valuable tool for research applications focused on cancer therapies, particularly in studies involving EGFR-dependent tumor growth and resistance mechanisms. -
EGFR Inhibitor
EGFR-IN-146 is an inhibitor of the epidermal growth factor receptor (EGFR) that disrupts EGFR signaling, effectively enhancing insulin sensitivity through AMPK pathway activation. This compound exhibits significant potential in reducing blood glucose levels and body weight. EGFR-IN-146 is valuable for research applications focused on diabetes and obesity, offering insights into metabolic regulation and potential therapeutic options. -
EGFR Inhibitor
DDC4002 is a selective inhibitor of the epidermal growth factor receptor (EGFR), targeting the L858R/T790M mutant subtype with an IC50 of 39 nM. This compound exhibits potent inhibitory activity, making it a valuable tool for cancer research, particularly in studies focused on therapeutic resistance in non-small cell lung cancer. Its application supports investigations into the mechanisms of EGFR-driven malignancies and offers insights into potential treatment strategies. -
EGFR Inhibitor
Paeciloquinone E is a selective inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. This compound demonstrates significant biological activity in modulating cell proliferation and survival pathways associated with EGFR signaling. It serves as a valuable tool in cancer research, particularly for studying the effects of EGFR inhibition in various tumor models. -
EGFR Inhibitor
NRC-2694-A is a potent orally bioavailable inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It exhibits significant activity against malignant squamous cell carcinoma (HNSCC), making it a valuable tool for researchers investigating EGFR-related signaling pathways and therapeutic strategies in cancer treatment. Its application in preclinical studies may enhance understanding of tumorigenesis and resistance mechanisms associated with EGFR inhibition. -
EGFR Inhibitor
PF-6422899 is a selective inhibitor of the epidermal growth factor receptor (EGFR) that exhibits binding affinity in the nanomolar range. It demonstrates potent biological activity against EGFR, making it a valuable tool in cancer research, particularly in studies focused on EGFR-driven pathways. Additionally, PF-6422899 may also interact with SOAT1, suggesting potential applications in the modulation of lipid metabolism in cancer cells. -
EGFR/ERBB2 Inhibitor
HKI-357 dimaleate is an irreversible dual inhibitor targeting EGFR and ERBB2, exhibiting IC50 values of 34 nM and 33 nM, respectively. This compound effectively suppresses EGFR autophosphorylation at tyrosine 1068, as well as the phosphorylation of downstream signaling molecules AKT and MAPK. HKI-357 dimaleate is primarily used in research to investigate mechanisms of oncogenesis and assess potential therapeutic strategies in cancer that involve EGFR and ERBB2 pathways. -
EGFR Inhibitor
Paeciloquinone F is a potent inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It has been demonstrated to effectively impede EGFR signaling pathways, making it a valuable tool for studies focused on cancer research and therapeutic development. The compound's ability to modulate EGFR activity facilitates investigations into tumor growth and progression, as well as the potential for targeted cancer therapies. -
EGFR Inhibitor
Paeciloquinone C is a potent inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. It effectively inhibits the V-abl protein tyrosine kinase with an IC50 value of 0.56 μM. This compound is utilized in research focused on cancer biology and targeted therapies, providing insights into the mechanisms of EGFR-mediated signal transduction. -
EGFR Inhibitor
1,2,3,4-Tetrahydro Staurosporin is a selective inhibitor of the mutant epidermal growth factor receptor (EGFR), particularly EGFRT790M, with an IC50 of 74 nM, demonstrating potential in targeting drug-resistant mutations. This compound also exhibits a higher IC50 of 390 nM against wild-type EGFR, highlighting its specificity. Additionally, 1,2,3,4-Tetrahydro Staurosporin interacts with Janus kinase 3 (JAK3), making it suitable for research applications focused on cancer biology and signaling pathways. -
EGFR/HER2 Mutant Inhibitor
EGFR-IN-99 is a potent inhibitor specifically targeting EGFR and HER2 Exon 20 insertion mutants. This compound exhibits exceptional antiproliferative activity in DFCI127 cells, with an EC50 value of 11.5 nM. EGFR-IN-99 is designed for research applications related to non-small cell lung cancer (NSCLC), making it a valuable tool for studying mutant-driven tumorigenesis and therapeutic resistance. -
EGFR Inhibitor
Paeciloquinone A is a selective inhibitor of the epidermal growth factor receptor (EGFR) protein tyrosine kinase. This compound demonstrates significant biological activity by inhibiting V-abl protein tyrosine kinase with an IC50 value of 0.59 μM. It is utilized in research for investigating EGFR-related signaling pathways and potential therapeutic applications in cancer treatment. -
EGFR Inhibitor
Paeciloquinone B is an inhibitor of the EGFR (epidermal growth factor receptor) protein tyrosine kinase. This compound demonstrates significant biological activity in obstructing EGFR signaling pathways, making it a valuable tool in cancer research, particularly for the study of tumor growth and proliferation. Its application in the investigation of specific cancer types associated with EGFR overexpression provides insights into potential therapeutic strategies. -
EGFR Inhibitor
LDC0496 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates strong inhibitory activity against both EGFR and Her2 exon 20 insertion mutations, while maintaining selectivity for wild-type EGFR and demonstrating minimal cross-reactivity within the kinome. This compound is valuable for research applications focused on targeted therapies in cancers associated with EGFR mutations. -
EGFR Inhibitor
EGFR-IN-9 is a potent inhibitor of the epidermal growth factor receptor (EGFR) kinase, exhibiting IC50 values of 7 nM for wild-type EGFR and 28 nM for the double mutant EGFR (L858R/T790M). This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research, particularly in studies focusing on EGFR-related pathways and mutations. It is suitable for investigations into therapeutic strategies targeting EGFR in various cancer models. -
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.
