Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
ADAM17 inhibitor
JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases. -
EGFR inhibitor
Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy. -
EGFRC797S inhibitor
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8 nM for EGFR^L858R/T790M/C797S, 6.8 nM for EGFR^WT, and 30.5 nM for EGFR^L858R/T790M. It exhibits potent antiproliferative activity and effectively suppresses tumor growth in vivo, making it a valuable tool for cancer research, particularly in the context of non-small cell lung carcinoma. -
EGFR inhibitor
Silevertinib (BDTX-1535, EGFR-IN-76) is an orally bioavailable, blood-brain barrier-permeable, and selective EGFR inhibitor with demonstrated antitumor activity. It has shown efficacy in preclinical models of non-small cell lung cancer (NSCLC), glioblastoma patient-derived tumors, and intracranial tumor models. -
EGFR inhibitor
Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor that suppresses tumor cell proliferation. It is primarily investigated for its potential in treating EGFR T790M-positive non-small cell lung cancer (NSCLC). -
EGFR inhibitor
O-Desmethyl gefitinib is an active plasma metabolite of gefitinib, formed via CYP2D6-mediated metabolism. It retains EGFR inhibitory activity with an IC50 of 36 nM in subcellular assays. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
EGFR inhibitor
Rezivertinib (BPI-7711) is an orally active, highly selective, and irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to potently target both common activating EGFR mutations and the resistance-associated T790M mutation, which is a frequent cause of acquired resistance to earlier-generation TKIs. Rezivertinib also demonstrates excellent central nervous system (CNS) penetration, making it effective against brain metastases in EGFR-mutant non-small cell lung cancer (NSCLC). With its strong antitumor activity and favorable pharmacokinetic profile, Rezivertinib is a promising candidate for the treatment of EGFR-mutant NSCLC, particularly in patients with CNS involvement or T790M-driven resistance. -
pan-ErbB inhibitor
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor targeting EGFR, HER2, and HER4. It potently inhibits ErbB family signaling pathways, suppressing tumor proliferation and survival. Dacomitinib hydrate is a valuable agent for research into cancers, particularly metastatic non-small cell lung cancer (NSCLC), where it demonstrates efficacy in targeting EGFR-driven oncogenesis. -
EGFR inhibitor
PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM. It targets the EGFR signaling pathway, which is critical for cell proliferation and survival in various cancers. PP 3 is a useful tool for research into EGFR-driven malignancies, such as non-small cell lung cancer and head and neck squamous cell carcinoma, enabling studies on tumor growth inhibition and potential therapeutic strategies. -
EGFR inhibitor
JBJ-09-063 hydrochloride is a highly potent, mutant-selective allosteric inhibitor of epidermal growth factor receptor (EGFR), specifically designed to target both TKI-sensitive and TKI-resistant EGFR mutations. It exhibits exceptionally low IC₅₀ values of: * 0.147 nM for EGFR L858R * 0.063 nM for EGFR L858R/T790M * 0.083 nM for EGFR L858R/T790M/C797S * 0.396 nM for EGFR^LT/L747S JBJ-09-063 hydrochloride effectively suppresses phosphorylation of EGFR and downstream signaling components, including Akt and ERK1/2, thereby inhibiting oncogenic signaling pathways. Its robust efficacy across a range of EGFR mutation profiles—including triple mutants that are resistant to third-generation TKIs—makes it a promising candidate for research and development in the treatment of EGFR-mutant non-small cell lung cancer (NSCLC). -
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
EGFR inhibitor
Limertinib (ASK120067) is a potent and orally active third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that selectively targets the EGFR^T790M resistance mutation with an IC₅₀ of 0.3 nM, while exhibiting reduced activity against wild-type EGFR (EGFR^WT, IC₅₀ = 6.0 nM). It is being investigated as a targeted therapy for non-small cell lung cancer (NSCLC) harboring EGFR-activating and resistance mutations. -
EGFR inhibitor
BLU-945 is a potent, highly selective, reversible, and orally bioavailable tyrosine kinase inhibitor (TKI) targeting mutant forms of the epidermal growth factor receptor (EGFR). It effectively inhibits EGFR variants harboring activating mutations such as L858R or exon 19 deletions, as well as resistance-associated mutations including T790M and C797S. BLU-945 is being developed as a next-generation therapeutic agent for the treatment of EGFR-mutant non-small cell lung cancer (NSCLC), particularly in cases resistant to earlier-generation EGFR inhibitors. -
EGFR inhibitor
CH7233163 is a noncovalent, ATP-competitive inhibitor that selectively targets the EGFR-Del19/T790M/C797S triple mutation, a known resistance mechanism to third-generation EGFR inhibitors such as Osimertinib. It effectively inhibits EGFR phosphorylation in Del19/T790M/C797S-mutant NIH3T3 cells and demonstrates significant antitumor activity in preclinical models. CH7233163 offers a promising therapeutic strategy for overcoming resistance in EGFR-mutant non-small cell lung cancer. -
ErbBs/BTK Inhibitor
Sunvozertinib (DZD9008) is a potent, orally active inhibitor of ErbB family kinases, including mutant forms of EGFR and HER2, as well as Bruton's tyrosine kinase (BTK). It demonstrates strong inhibitory activity against a range of clinically relevant EGFR mutations, with IC₅₀ values of 20.4 nM for EGFR exon 20 NPH insertion, 20.4 nM for EGFR exon 20 ASV insertion, 1.1 nM for EGFR L858R/T790M, and 7.5 nM for HER2 exon 20 YVMA mutation. It exhibits reduced activity against wild-type EGFR (IC₅₀ = 80.4 nM in A431 cells), supporting its selectivity for mutant forms. Sunvozertinib is being investigated as a targeted therapy for non-small cell lung cancers harboring EGFR or HER2 exon 20 alterations. -
EGFR inhibitor
Asandeutertinib (Osimertinib-d₃; AZD-9291-d₃) is a deuterated analog of Osimertinib, functioning as a tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR). It retains potent antineoplastic activity and is primarily used in research settings to study EGFR-driven cancers, particularly non-small cell lung cancer (NSCLC) with EGFR mutations, while offering potential advantages in pharmacokinetics due to deuterium substitution. -
EGFR inhibitor
(E)-AG 556 is a highly selective inhibitor of epidermal growth factor receptor (EGFR) that also exhibits anti-inflammatory activity by blocking lipopolysaccharide (LPS)-induced tumor necrosis factor-alpha (TNF-α) production. Its dual functionality makes it a valuable compound for investigating EGFR-driven signaling pathways as well as inflammation-related mechanisms. -
EGFR inhibitor
Pebezertinib (BLU-451) is an orally bioavailable epidermal growth factor receptor (EGFR) inhibitor with demonstrated central nervous system (CNS) penetration. It is specifically designed to target EGFR mutations, including exon 20 insertions, and is being investigated for the treatment of non-small cell lung cancer (NSCLC) harboring these alterations. Pebezertinib represents a promising therapeutic candidate for overcoming resistance in EGFR-driven NSCLC, particularly in cases with CNS involvement. -
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.
