Catalog No.
Product Name
Application
Product Information
Citations
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EGFR Inhibitor
EGFR-IN-50 is a potent inhibitor of the epidermal growth factor receptor (EGFR), specifically targeting the L858R resistance mutation. It exhibits strong anti-proliferative activity in cancer cells, with a GI50 of 8 nM against TEL-EGFR-L858R-BaF3 cells and 6.03 μM against TEL-EGFR-T790M-L858R-BaF3 cells. This compound is valuable for research applications focused on overcoming resistance in EGFR-driven cancers. -
EGFR Inhibitor
NSC381467 is a potent, orally active inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. This compound exhibits significant antiproliferative activity, making it a valuable tool in cancer research. NSC381467 is suitable for studies aimed at understanding EGFR-mediated signaling pathways and their implications in tumor biology. -
VEGFR Inhibitor
Jaceidin is a selective vascular endothelial growth factor receptor (VEGFR) inhibitor that demonstrates significant anti-tumor activity. This compound is characterized by its excellent membrane permeability and oral bioavailability, making it a valuable candidate for further research. Jaceidin holds potential for applications in cancer therapy, particularly in inhibiting angiogenesis associated with tumor growth. -
Src Kinase Inhibitor
SKS-927 is a potent Src kinase inhibitor with an IC50 value of 3.9 nM, demonstrating significant inhibition of Src-transformed cell proliferation in rat fibroblasts, with an IC50 of 73 nM. Additionally, SKS-927 shows activity against EGFR at an IC50 of 720 nM. This compound is applicable in research focused on cancer and osteoporosis, making it a valuable tool for investigating therapeutic pathways in these conditions. -
EGFR Inhibitor
EGFR-IN-179 is a selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 0.068 μM for the EGFR L858R/T790M/C797S mutant and 2.56 μM for wild-type EGFR. This compound exhibits significant anticancer activity, particularly against non-small cell lung cancer, making it a valuable tool for research into targeted therapies and understanding resistance mechanisms in cancer treatment. -
EGFR Inhibitor
EGFR-IN-451 is a potent EGFR inhibitor, demonstrating an IC50 value of 0.02 nM. This compound effectively targets mutant variants of EGFR, including EGFRL858R, EGFRT790M, and EGFRL858R/T790M, with IC50 values ranging from 0.26 to 34 nM. EGFR-IN-451 significantly inhibits the activation of downstream signaling proteins AKT and ERK, leading to reduced proliferation in EGFR-mutant cancer cell lines. It is suitable for research focused on EGFR-driven malignancies. -
EGFR Inhibitor
Z118332870 is a potent inhibitor of the epidermal growth factor receptor (EGFR) and bromodomain-containing protein 4 (BRD4). This compound displays significant antitumor activity, making it a promising candidate for addressing resistance mechanisms in cancer therapy. Its dual targeting capability may enhance therapeutic efficacy in various cancer types. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
EGFR/HER2/DHFR Inhibitor
EGFR/HER2/DHFR-IN-1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and dihydrofolate reductase (DHFR). This compound demonstrates potent antitumor efficacy, with IC50 values of 0.153 μM for EGFR, 0.108 μM for HER2, and 0.291 μM for DHFR. EGFR/HER2/DHFR-IN-1 effectively arrests the cell cycle at the G1/S phase and promotes apoptosis in MCF-7 breast cancer cells, making it a valuable reagent for cancer research and therapeutic development. -
EGFR Inhibitor
SIQ17 is a potent inhibitor of the epidermal growth factor receptor (EGFR) that acts by binding to the ATP-binding site, exhibiting an IC50 of 0.62 nM. This compound demonstrates superior inhibitory activity against EGFR tyrosine kinase compared to Erlotinib, which has an IC50 of approximately 20 nM. SIQ17 is applicable in cancer research, particularly in studies focusing on EGFR-mediated signaling pathways and therapeutic resistance. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-3 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 191.08 nM, 132.65 nM, and 113.98 nM, respectively. This compound demonstrates significant antitumor activity, making it valuable for research in cancer therapies and signaling pathways involving these targets. Its inhibitory effects on cell proliferation in cancer models may aid in the understanding and development of targeted treatment strategies. -
EGFR Inhibitor
HNPMI is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting cytotoxic effects on cancer cells. This compound disrupts the expression of key proteins, including osteopontin, survivin, and cathepsin S, ultimately promoting apoptosis. Additionally, HNPMI influences the BCL-2/BAX ratio and p53 pathways in colorectal cancer cell lines, contributing to the inhibition of tumorigenesis and providing valuable insights for cancer research. -
EGFR Inhibitor
EGFR-IN-27 is a highly effective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of less than 50 nM against various mutations, including EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S. This compound is essential for research focused on targeted cancer therapies, particularly in understanding the mechanisms of resistance in non-small cell lung cancer. Its specificity for multiple EGFR mutations makes it a valuable tool for investigating pathways associated with tumor progression and treatment response. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-1 is a highly active inhibitor of EGFR, HER2, and CDK9, displaying IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively. This compound demonstrates significant antitumor properties, making it a valuable tool for cancer research. Its ability to target multiple kinases involved in cell proliferation and survival pathways supports investigations into therapeutic strategies for various malignancies. -
EGFR Inhibitor
EGFR-IN-30 is a highly potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values in the range of 1-10 nM and less than 1 nM for both wild-type EGFR and mutant forms (L858R/T790M/C797S). Its strong inhibitory activity positions EGFR-IN-30 as a valuable reagent for investigating cell proliferative diseases, particularly in cancer research applications where modulation of the EGFR signaling pathway is essential. -
EGFR Inhibitor
EGFR-IN-102 is a potent inhibitor of the epidermal growth factor receptor (EGFR), displaying an IC50 value of 2 nM. This compound is designed for oral administration and shows significant activity in the study of non-small-cell lung cancer (NSCLC). Its selectivity and efficacy make it a valuable tool for research focused on targeting EGFR-driven tumorigenesis and exploring therapeutic strategies in cancer treatment. -
EGFR Inhibitor
EGFR-IN-32 is a potent inhibitor of the epidermal growth factor receptor (EGFR). Activation and dysregulation of EGFR are implicated in the uncontrolled proliferation of cells and the advancement of numerous cancers, particularly non-small cell lung cancer (NSCLC). This compound is valuable for research into diseases driven by EGFR mutations, facilitating investigations into therapeutic interventions targeting this oncogenic pathway. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-10 is a selective dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting IC50 values of 2.3 nM and 234 nM for EGFR and HER2, respectively. This compound demonstrates significant antiproliferative effects against prostate carcinoma, making it a valuable tool for research in cancer biology and targeted therapy development. Its specificity for both EGFR and HER2 positions it as a promising candidate for further investigations into dual receptor inhibition and its therapeutic potential. -
EGFR Inhibitor
JGK-068S is a potent EGFR inhibitor that specifically targets the epidermal growth factor receptor. This compound demonstrates significant biological activity by effectively blocking the signaling pathways associated with tumor growth and proliferation. JGK-068S is commonly utilized in cancer research to investigate its therapeutic potential and mechanisms of action in EGFR-driven malignancies. -
EGFRL858R/T790M Inhibitor
EGFR T790M/L858R-IN-4 is a targeted inhibitor specifically designed to block the mutated forms of the epidermal growth factor receptor (EGFR) associated with non-small cell lung cancer (NSCLC), namely L858R and T790M mutations. This compound exhibits significant anticancer activity, making it a valuable tool for research on targeted therapies and resistance mechanisms in cancer treatment. It is particularly useful in studying drug resistance and evaluating potential therapeutic strategies in EGFR-driven tumor models. -
EGFR Inhibitor
EGFR-IN-189 is a selective covalent inhibitor of the epidermal growth factor receptor (EGFR), with an IC50 value of 200 nM. This compound effectively targets the C797S mutant form of EGFR, demonstrating potent inhibition of cancer cell proliferation. Furthermore, EGFR-IN-189 disrupts EGFR phosphorylation and subsequently inhibits ERK1/2 phosphorylation, making it a valuable tool for research applications in non-small cell lung cancer. -
EGFR Inhibitor
EGFR-IN-33 is a selective inhibitor of the epidermal growth factor receptor (EGFR), designed to target aberrant signaling pathways associated with tumor growth. This acrylamide derivative exhibits significant anti-tumor activity while maintaining low toxicity profiles. EGFR-IN-33 is particularly relevant for research focusing on cancers driven by EGFR mutations and overexpression, including non-small cell lung cancer (NSCLC). Its potential utility in elucidating the mechanisms of EGFR-related malignancies establishes it as a valuable tool in cancer research. -
EGFR TKI
EGFR-IN-23 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 8.05 nM in BaF3 cells expressing the EGFR-DEL19/T790M/C797S mutation. This compound demonstrates significant effectiveness in inhibiting cell proliferation associated with oncogenic EGFR signaling. EGFR-IN-23 is suitable for research applications focused on cancer biology, particularly in studies investigating resistance mechanisms in targeted therapies. -
EGFR Inhibitor
EGFR-IN-49 is a selective inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 65.0 nM for EGFRT790M and 13.6 nM for EGFRT790M/L858R variants. This compound effectively induces late apoptosis in a dose-dependent manner, making it a valuable tool for studying cancer cell signaling and apoptosis mechanisms. Its potency and selectivity position EGFR-IN-49 as a promising reagent for research applications focused on targeting EGFR-related pathways in cancer therapeutics. -
EGFR Kinase Inhibitor
EGFR-IN-112 is a potent inhibitor of the EGFR kinase, exhibiting IC50 values of 2.31 ± 0.3 μM in MCF-7, 3.16 ± 0.8 μM in H69AR, and 4.2 ± 0.2 μM in PC-3 cancer cell lines. This compound shows selective cytotoxicity towards cancer cells, making it a valuable tool for research in targeted cancer therapies and investigations into EGFR-related signaling pathways. Its efficacy highlights its potential in the study of cancer resistance mechanisms and the development of novel anticancer treatments. -
EGFR Inhibitor
BIEGi-1 is a selective inhibitor of the epidermal growth factor receptor (EGFR), primarily targeting the inhibition of EGFR-Rheb interactions within cells. It significantly suppresses EGFR kinase activity, as evidenced by reduced levels of p-Y1068-EGFR, and also impedes mTORC1 activation by lowering p-T389-S6K1 levels in EGFR-mutant cell lines. BIEGi-1 demonstrates pronounced antiproliferative effects on EGFR-mutant PC9 and HCC827 cells, exhibiting IC50 values of 17 nM and 20 nM, respectively. This compound is a valuable tool for investigating cancers associated with EGFR mutations, notably non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR-IN-199 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 1.1 nM and 1.4 nM for purified EGFR wild-type and EGFRT790M/L858R kinases, respectively. This compound is valuable for cancer research, particularly in studies focused on EGFR signaling pathways and resistance mechanisms in tumor biology. -
EGFR Del19 Inhibitor
EGFR-IN-73 is a selective inhibitor targeting the EGFR Del19 mutation, demonstrating an IC50 value of 119 nM. This compound exhibits potent inhibition of tumor proliferation driven by the prevalent EGFR Del19 mutation. It is suitable for research applications focusing on cancer biology and therapeutic development for EGFR-driven malignancies. -
EGFR Ligand
EGFR ligand-2 (compound C4) is a covalent inhibitor targeting the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 21 nM for the EGFRL858R mutant and 48 nM for the EGFRL858R/T790M double mutant. This compound is useful in studying EGFR mutations associated with various cancers and can be utilized in the synthesis of PROTACs for targeted protein degradation research applications. -
EGFR Inhibitor
NS-062 is an orally active, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates significant antiproliferative activity in drug-resistant double mutated H1975 cells, with an IC50 value of 0.19 μM. Furthermore, NS-062 shows antitumor efficacy in an H1975 mouse xenograft model, making it a valuable tool for research on EGFR-related cancer treatments. -
EGFR Inhibitor
Gefitinib N-oxide is an N-oxide derivative of Gefitinib, acting as an inhibitor of the epidermal growth factor receptor (EGFR). It demonstrates a potent inhibitory effect, with an IC50 range of 2-37 nM in NR6wtEGFR cells. This compound is primarily utilized in research to investigate the modulation of EGFR signaling pathways and its implications in various cancer models. -
EGFR Inhibitor
EGFR-IN-35 is a selective inhibitor of the epidermal growth factor receptor (EGFR), known for its role in regulating cell growth. This acrylamide derivative exhibits potent anti-tumor activity while maintaining a favorable safety profile. It is particularly relevant for studying cancers characterized by EGFR overexpression or mutations, such as non-small cell lung cancer (NSCLC). EGFR-IN-35 serves as a valuable tool for research into targeted therapies and mechanisms underlying EGFR-related oncogenesis. -
EGFR Inhibtior
EGFR-IN-21 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 of 0.38 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its efficacy in inhibiting EGFR signals positions it for applications in studies focused on oncogenic pathways and targeted cancer treatments. -
EGFR Inhibtior
EGFR-IN-28 is a potent inhibitor of the epidermal growth factor receptor (EGFR). This compound exhibits significant antitumor activity, making it a valuable tool in cancer research. EGFR-IN-28 is primarily utilized to study the mechanisms of tumor growth and response to targeted therapies in various malignancies. -
EGFR/CDK-2 Inhibitor
EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival. -
EGFR/BRAF Inhibitor
EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development. -
pan-HER Inhibitor
BMS-599626 dihydrochloride is a small molecule pan-HER inhibitor that targets the human epidermal growth factor receptor family, specifically inhibiting HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activities. This compound functions by competing with ATP for binding to these receptors, thereby blocking their kinase activity and downstream signaling pathways through the inhibition of heterodimer formation between HER1 and HER2. BMS-599626 dihydrochloride serves as a valuable tool for investigating the antitumor effects in various tumor models overexpressing HER1 and HER2. -
EGFR Inhibitor
EGFR-IN-139 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 12.88 nM for wild type, 10.84 nM for L858R/T790M, and 42.68 nM for L858R/T790M/C797S mutants. This compound exhibits significant anticancer activity in A549 and H1975 cell lines, demonstrating strong selectivity for cancer cells that overexpress EGFR. EGFR-IN-139 is particularly relevant for research focused on nonsmall cell lung cancer (NSCLC). -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-5 is an orally active irreversible dual inhibitor targeting the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). It exhibits a potent inhibitory effect on EGFR with an IC50 value of 1.01 nM and effectively inhibits EGFR kinase activity associated with L858R and T790M mutations. This compound demonstrates significant antitumor efficacy in vivo, making it a valuable tool for lung cancer research and the development of targeted therapies in oncology. -
EGFR Inhibitor
JBJ-07-149 is a potent EGFR inhibitor targeting the L858R/T790M mutations, exhibiting an IC50 of 1.1 nM. This compound effectively inhibits the proliferation of Ba/F3 cells, showing IC50 values of 4.9 μM and 0.148 μM in the absence and presence of Cetuximab, respectively. JBJ-07-149 serves as a useful ligand for the synthesis of DDC-01-163, facilitating research on EGFR-related pathways and therapeutic interventions in cancer. -
PROTAC EGFR Degrader
PROTAC EGFR Degrader 13 is a targeted protein degradation compound that selectively degrades the epidermal growth factor receptor (EGFR). This degrader exhibits potent antiproliferative activity with an IC50 of 15.6 nM against Ba/F3 cells harboring the EGFR T790M-L858R-C797S mutations, demonstrating its effectiveness in EGFR-related cancer research. This reagent is suitable for investigating the underlying mechanisms of EGFR-driven malignancies and developing therapeutic strategies focused on targeted degradation pathways. -
EGFR/VEGFR-2 Inhibitor
EGFR-IN-121 is a potent dual inhibitor targeting EGFR and VEGFR-2, exhibiting IC50 values of 84 nM and 3.5 nM, respectively. This compound demonstrates significant biological activity that can impede tumor growth and angiogenesis by inhibiting key signaling pathways associated with cancer progression. EGFR-IN-121 is suitable for research applications focused on cancer therapeutics, particularly in evaluating the effects of EGFR and VEGFR-2 inhibition in various cancer models. -
EGFR Inhibitor
PKI-166 hydrochloride is a selective and potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 value of 0.7 nM. This compound is primarily utilized in cancer research, particularly in studies focused on EGFR-driven tumors. Its effectiveness in inhibiting EGFR activity makes it a valuable tool for investigating targeted therapies and understanding signaling pathways in oncogenesis. -
EGFR/HER2 Inhibitor
EGFR/HER2-IN-11 is a potent dual inhibitor targeting the human epidermal growth factor receptors HER2 and EGFR, demonstrating IC50 values of 7.7 nM and 22 nM, respectively. This compound exhibits significant antitumor activity and effectively inhibits the proliferation of cancer cells, specifically showing a GI50 of 601 nM against the BT-474 cell line. EGFR/HER2-IN-11 is suitable for research applications focused on cancer biology and therapeutic development targeting these key oncogenes. -
EGFR Inhibitor
CGP-59326 is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 0.027 μM. This compound effectively disrupts the EGFR signaling pathway, exhibiting strong inhibition of EGFR-dependent tumor cells. CGP-59326 is valuable for research applications in cancer biology, particularly in studies investigating EGFR-related malignancies. -
EGFR/c-Met Inhibitor
EGFR/c-Met-IN-1 is a dual inhibitor targeting both EGFR and c-Met, with IC50 values of 68.1 nM for EGFRL858R and 0.26 nM for c-Met. This compound induces apoptosis and causes cell cycle arrest in A549-P cells by downregulating the phosphorylation of EGFR, c-Met, and downstream AKT pathways. EGFR/c-Met-IN-1 demonstrates significant tumor growth inhibition in vitro and in vivo, making it a valuable reagent for cancer research focused on targeting these pathways. -
EGFR Inhibitor
EGFR-IN-71 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting an IC50 value of 3.7 μM. This compound is particularly useful in research focused on chordoma, providing a tool for studying EGFR-related signaling pathways. Additionally, EGFR-IN-71 features an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling diverse applications in chemical biology and bioconjugation studies. -
EGFR Inhibitor
EGFR-IN-193 is an inhibitor of the Epidermal Growth Factor Receptor (EGFR), primarily utilized in the synthesis of PROTACs as target protein ligands. It serves as a crucial component in the development of novel protein degradation strategies, particularly exemplified by PROTAC EGFR degrader 17, facilitating studies in cancer biology and targeted therapy research. This compound enables the exploration of EGFR signaling pathways and their roles in oncogenesis and tumor progression. -
EGFR-C797S Inhibitor
EGFR/C797S-IN-1 is a selective inhibitor targeting the EGFR-C797S variant, demonstrating an IC50 of 0.128 µM. This compound exhibits significant anti-proliferative and anti-tumor effects, making it a valuable tool for cancer research. Notably, EGFR/C797S-IN-1 inhibits the phosphorylation of EGFR in a dose-dependent manner, contributing to its potential in therapeutic applications against resistant tumor phenotypes. -
EGFR Modulator
CHNQD-01281 is an EGFR modulator that exhibits potent antiproliferative activity against cancer cells, with IC50 values of 0.079 and 0.081 μM for T24 and J82 cell lines, respectively. This compound effectively regulates both the EGFR/PI3K/AKT and EGFR/ERK signaling pathways, enhancing the chemotactic response of immune effector cells to chemokines. In vivo studies demonstrate that CHNQD-01281 significantly inhibits tumor growth in T24 xenograft mouse models and extends survival in MB49 allogeneic mouse models by promoting the infiltration of cytotoxic T cells.
