EGFR Inhibitor

TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.

EGFR-IN-126 (compound 9d) is a potent inhibitor of EGFR^{L858R/T790M/C797S}, with the IC₅₀ value of 0.005 μM. EGFR-IN-126 shows antitumor effects in vivo and in vitro.

EGFR/Cytokine-IN-1 is an EGFR (IC₅₀ = 0.03 μM) and Cytokine inhibitor (TNF-α, IC₅₀ = 3.1 μM; IL-6, IC₅₀ = 1.6 μM). EGFR/Cytokine-IN-1 shows potent anticancer activity on A549 and MCF7, respectively. EGFR/Cytokine-IN-1 significantly reduces IL-6 and TNF-α levels in A549 cells, and also shows promising ADMET profiles. EGFR/Cytokine-IN-1 can induce apoptosis in a dose-dependent manner. compound 5h can be used for the study of breast cancer and lung cancer.

EGFR-IN-203 is a EGFR kinase domain inhibitor targeting EGFR^{T790M/C797S/V948R}. EGFR-IN-203 stably binds to the allosteric pocket of EGFR in an inactive conformation. EGFR-IN-203 can be used in research related to cancers such as non-small cell lung cancer.

HB-EGF-IN-1 is a HB-EGF inhibitor. HB-EGF-IN-1 can be used for lung squamous cell carcinoma research.

EGFR T790M/L858R-IN-5 (example 52) is a potent inhibitor of EGFR T790M/L858R with the inhibition percentage of 92.9% in the concerntration of 0.05 μM.

EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR^T790M.

EGFR T790M/L858R-IN-3 (compound B1) is a EGFR^L858R/T790M inhibitor with IC₅₀ value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC₅₀ value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells.

EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity.

TAT-327 is cell-penetrating peptide. TAT-327 selectively inserts into cancer cell membranes and shows potent antitumor activity. TAT-327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. TAT-327 significantly inhibits tumor growth in HT-29 xenograft mcie models.

EGFR-IN-68 (Compound 8d) is a potent EGFR inhibitor with an IC₅₀ of 0.33 μM. EGFR-IN-68 shows anticancer activity.

EGFR/Akt-IN-1 (compound 17) is a potent inhibitor of EGFR/Akt, with the IC₅₀s of 12.89 μM and 10.88 μM in A549 cells, respectively. EGFR/Akt-IN-1 arrestes the cell cycle at the S phase.

Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).

Delphinidin 3-glucoside (chloride) (Standard) is the analytical standard of Delphinidin 3-glucoside (chloride). This product is intended for research and analytical applications. Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL). Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC50 of 9.7 μM. Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC50 of 2.37 µM. Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction.

Cetuximab sarotalocan (RM-1929) is an IRdye700DX (near-infrared photosensitizing dye) conjugate of Cetuximab (anti-EGFR monoclonal antibody). Cetuximab sarotalocan can be used for head and neck cancers research.

RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.

EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12).

EGFR-IN-39 is a potent inhibitor of EGFR. EGFR-IN-39 is an anti-tumor agent with low toxic side effects. EGFR-IN-39 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-39 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 2).

EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR^{L858R/T790M/C797S} and BaF3–^{C797S/Del19/T790M}, with IC₅₀ of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models.

EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC₅₀: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC₅₀ of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis.