EGFR Inhibitor

EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC.

PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.

Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC₅₀s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively.

KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative.

NP1 peptide is a cyclic peptide (CHSHGTRAC) and TK-EGFR inhibitor (IC₅₀ = 0.58 nM, K_d = 18.40 μM). NP1 peptide blocks kinase activity by binding to the ATP-binding pocket of TK-EGFR and inhibits autophosphorylation at the EGFR Y1173 site, and it also serves as a pH-responsive nanocarrier for siRNA delivery. NP1 peptide is used in cancer research.

EGFR-IN-195 is a EGFR inhibitor with an IC₅₀ of 0.89 nM. EGFR-IN-195 inhibits the viability of breast cancer cells. EGFR-IN-195 can be used in breast cancer-related research.

EGFR-IN-148 (compound 8c) is a potent inhibitor of EGFR , with the IC₅₀ of 0.161 μM. EGFR-IN-148 causes G1/S arrest and markedly enhances apoptosis in HepG2 cells.

UNC-CA359 is a potent epidermal growth factor receptor (EGFR) inhibitor, with an IC₅₀ value of 18 nM. UNC-CA359 exhibits strong anti-tumor activity, can be used to Chordoma research. UNC-CA359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC₅₀ of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC₅₀ values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS.

Gefitinib N-oxide hydrochloride is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC₅₀ of 2-37 nM in NR6wtEGFR cells.

EGFR-IN-79 (compound 21) is an EGFR inhibior with antitumor activity. EGFR-IN-79 induces ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. EGFR-IN-79 induces cell death at both proliferating and quiescent zones of EJ28 spheroids. EGFR-IN-79 exhibits safety profile in the zebrafish-based model.

Anti-Epiregulin Antibody is an anti-Epiregulin antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research.

EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC₅₀ value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research.

Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.

EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase.

NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC₅₀ of 0.15 nM. NSC81111 has anticaner effects.

Paeciloquinone D can inhibit the EGFR protein tyrosine kinase.

BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells.