DesMethyl Erlotinib HCl

DesMethyl Erlotinib HCl (CAS No.: 183320-51-6) is an EGFR inhibitor derived from the major active metabolite of erlotinib (also known as OSI-420), and is commonly used in scenarios such as target validation, mechanism-of-action analysis, and lead compound optimization. By inhibiting the catalytic activity of epidermal growth factor receptor (EGFR) tyrosine kinase and attenuating ligand-induced receptor autophosphorylation, it modulates downstream signaling cascades such as RAS–RAF–MEK–ERK and PI3K–AKT, providing a controllable intervention for studying proliferation- and survival-related signaling readouts in EGFR-dependent model systems; in in vitro assays, enzymatic inhibition typically appears at low nanomolar levels, while inhibition of receptor phosphorylation in cells is often observed in the single-digit to tens of nanomolar range, and may extend from the nanomolar to low micromolar range depending on experimental conditions. This molecule is compatible with bioorthogonal chemical labeling workflows, owing to its alkyne site that can undergo copper-catalyzed azide–alkyne cycloaddition (CuAAC), and can be used for studies such as chemical proteomics, imaging tracing, and target occupancy assessment without altering its core inhibitory function. Typical applications include serving as a reference control or comparative standard at the biochemical and cellular levels for quantitative analysis of EGFR phosphorylation kinetics, pathway mapping in combination with phosphoproteomics, support for structure–activity relationship studies of next-generation inhibitors, and experimental protocols evaluating synergistic effects with parallel signaling modulators in cell models and mechanism-oriented animal models; the concentration or dose used in experiments generally depends on the specific experimental design and research objectives. This product is for laboratory research use only.