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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. -
VEGFR Inhibitor
Gamabufotalin is a selective inhibitor of the Vascular Endothelial Growth Factor Receptor (VEGFR). This compound, derived from the traditional Chinese medicine Chansu, exhibits potent anti-cancer properties by significantly suppressing cancer cell proliferation and modulating inflammatory responses. Its ability to inhibit angiogenesis is primarily attributed to the blockade of VEGFR-2 signaling pathways, making it a valuable tool for research in cancer therapies and vascular biology. -
PDGFR Inhibitor
Sennoside B is a potent inhibitor of platelet-derived growth factor receptor (PDGFR). It effectively suppresses cell proliferation and reduces the phosphorylation of PDGFR-β, STAT-5, AKT, and ERK in response to PDGF-BB stimulation. Additionally, Sennoside B exhibits gastroprotective properties and is suitable for research applications focused on gastritis and related gastrointestinal disorders. -
Bcr-Abl Inhibitor
Nilotinib hydrochloride is a potent Bcr-Abl tyrosine kinase inhibitor that exhibits significant antineoplastic activity. It is primarily utilized in research related to chronic myelogenous leukemia (CML), providing valuable insights into the molecular mechanisms of this disease and potential therapeutic strategies. Its oral bioavailability makes it a convenient choice for in vitro and in vivo studies focused on targeting the Bcr-Abl fusion protein. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
FLT3 Inhibitor
Dovitinib lactate hydrate is a multi-targeted tyrosine kinase inhibitor primarily targeting FLT3. It exhibits potent inhibitory activity with IC50 values of 1 nM for FLT3, making it a valuable tool for research in hematological malignancies. In addition to FLT3, it also inhibits c-Kit, FGFR1/3, VEGFR1/2/3, and PDGFRα/β, facilitating studies focused on various signaling pathways and cancer therapeutics. -
Syk Inhibitor
Syk Inhibitor II dihydrochloride dihydrate is a selective and ATP-competitive inhibitor of Syk with an IC50 of 41 nM. This compound effectively inhibits 5-HT release from RBL cells, demonstrating an IC50 of 460 nM. With reduced potency against other kinases, it holds potential for applications in treating allergic responses and exploring the role of Syk in various immunological processes. -
Syk Inhibitor
Syk Inhibitor II hydrochloride is a highly selective ATP-competitive inhibitor of Syk kinase, exhibiting an IC50 of 41 nM. This compound effectively inhibits serotonin release from RBL cells, with an IC50 of 460 nM. Syk Inhibitor II hydrochloride demonstrates reduced potency against other kinases, making it a valuable tool for investigating Syk-mediated signaling pathways and exploring its anti-allergic properties in research applications. -
FLT3 Inhibitor
CHMFL-FLT3-122 is a selective FLT3 kinase inhibitor with an IC50 of 40 nM. It demonstrates significant selectivity for FLT3 over BTK and c-KIT, exhibiting IC50 values of 421 nM and 559 nM, respectively. This compound effectively induces apoptosis through cell cycle arrest in the G0/G1 phase, making it a valuable tool for research in hematological malignancies and targeted cancer therapies. -
FLT3 Inhibitor
Tandutinib hydrochloride is a potent and selective inhibitor of FLT3, with an IC50 of 0.22 μM. This compound also exhibits inhibitory activity against c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. Its primary applications include research in acute myelogenous leukemia (AML). Additionally, Tandutinib hydrochloride demonstrates the ability to cross the blood-brain barrier, making it a valuable tool in studying central nervous system involvement in malignancies. -
BTK Inhibitor
XMU-MP-3 is a potent non-covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 10.7 nM for wild-type BTK and 17.0 nM for the C481S mutation in the presence of 10 μM ATP. This compound is known to induce apoptosis in BTK-dependent cells, making it a valuable tool for investigating B-cell receptor signaling and related pathways. XMU-MP-3 is applicable in research focused on hematological malignancies and immune responses. -
JAK2/FLT3 Inhibitor
Flonoltinib TFA is a potent and orally bioavailable inhibitor that targets both JAK2 and FLT3, exhibiting IC50 values of 0.7 nM and 4 nM, respectively, alongside 26 nM and 39 nM for JAK1 and JAK3. This compound possesses significant anti-cancer activity, making it a valuable tool for research in oncology and therapeutic development against malignancies driven by these pathways. Its dual inhibition profile highlights its potential in addressing cancers associated with aberrant JAK2 and FLT3 signaling. -
PDGFRα/β/Bcr-Abl Inhibitor
GZD856 formic is a selective inhibitor of PDGFRα/β, displaying IC50 values of 68.6 nM and 136.6 nM, respectively, along with potent inhibition of Bcr-Abl, including the T315I mutant with IC50s of 19.9 nM and 15.4 nM. This compound exhibits notable antitumor activity, making it a valuable tool for cancer research. Additionally, GZD856 formic serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation studies and compound labeling. -
BCR-ABL Inhibitor
S116836 is a potent BCR-ABL tyrosine kinase inhibitor that effectively targets both wild-type and T315I BCR-ABL variants. It induces apoptosis and arrests the cell cycle in the G0/G1 phase, promoting increased reactive oxygen species (ROS) and reduced glutathione (GSH) levels in BaF3/WT and BaF3/T315I cells. Additionally, S116836 inhibits SRC, LYN, HCK, LCK, BLK, as well as receptor tyrosine kinases including FLT3, TIE2, KIT, and PDGFR-β, demonstrating significant antitumor activity. This compound also features an alkyne group, making it suitable for click chemistry applications, particularly the copper-catalyzed azide-alkyne cycloaddition (CuAAc). -
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/VEGFR2 Inhibitor
EGFR/VEGFR2-IN-4 is an irreversible inhibitor targeting the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor 2 (VEGFR-2). It exhibits potent inhibitory activity with IC50 values of 18.7 nM for EGFR and 102.3 nM for VEGFR-2 in the presence of 1 μM ATP. This compound is valuable for research applications focused on cancer therapeutics and angiogenesis, providing insights into signaling pathways and potential treatment strategies. -
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. -
VEGFR iInhibitor
ZM-306416 hydrochloride is a potent inhibitor of vascular endothelial growth factor receptor (VEGFR), demonstrating IC50 values of 0.1 μM for KDR and 2 μM for Flt. In addition, it functions as an epidermal growth factor receptor (EGFR) inhibitor with an IC50 of less than 10 nM. This dual inhibition profile makes ZM-306416 hydrochloride valuable for research in cancer biology and angiogenesis, providing insights into tumor growth and vascular development mechanisms. -
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.
