Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
EGFR and HER2 inhibitors act on two closely related receptor tyrosine kinases of the ErbB family. The epidermal growth factor receptor (EGFR, ErbB1) and human epidermal growth factor receptor 2 (HER2, ErbB2) form dimers with each other and with ErbB3 and ErbB4. Receptor activation engages the mitogen-activated protein kinase (MAPK) and phosphoinositide 3-kinase (PI3K) pathways that control cell growth. Activating EGFR mutations in non-small-cell lung cancer have made the receptor a central model in kinase inhibitor research. Gefitinib and erlotinib are reversible EGFR inhibitors, and lapatinib inhibits both EGFR and HER2. Osimertinib binds covalently to EGFR carrying the T790M resistance mutation, and neratinib irreversibly inhibits HER2 and EGFR.
VEGFR-IN-4 is a potent epidermal growth factor receptor (EGFR) inhibitor. It demonstrates significant antiproliferative activity, exhibiting an IC50 value of 24.6 nM against HCC827 cells. This compound is primarily utilized in research focused on cancer therapeutics, particularly in studies exploring EGFR-mediated signaling pathways and tumor growth inhibition.
Out of stock
All 3 sizes
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.
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.
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.
Out of stock
All 3 sizes
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.
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.
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-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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
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-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.
Out of stock
All 3 sizes
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-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.
HER2-IN-13 is a selective HER2 inhibitor with an IC50 of 8 nM, demonstrating potent inhibition of the HER2 receptor. Additionally, it also inhibits wild-type EGFR with an IC50 of 0.40 μM. This compound is valuable for research applications focused on cancer biology, specifically in studying HER2-driven tumors and EGFR-related pathways.
Out of stock
All 3 sizes
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-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-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.
Synonyms: AZD-8931 fumarate
Sapitinib fumarate is a reversible, ATP-competitive inhibitor of the ErbB family, specifically targeting EGFR, ErbB2, and ErbB3 with IC50 values of 4 nM, 3 nM, and 4 nM, respectively. This compound exhibits potent inhibition of cellular proliferation driven by aberrant ErbB signaling pathways. It is commonly employed in research focused on cancer biology, particularly in studies investigating therapeutic resistance and receptor tyrosine kinase signaling.
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.
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.
Out of stock
All 3 sizes
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.
Out of stock
All 3 sizes
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.
HER2-IN-21 is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2), exhibiting an IC50 value of 3.85 μM. This compound is valuable for research focusing on HER2-positive cancers, including breast and gastric cancers. HER2-IN-21 is utilized in studies aimed at understanding HER2 signaling pathways and evaluating the efficacy of targeted therapies in cancer treatments.
Out of stock
All 3 sizes
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.
