Properties

Safety Information

Description

Erlotinib-d₆ (hydrochloride) contains six deuterium atoms located on the methoxy group. It is intended for use as an internal standard for the quantification of erlotinib by GC- or LC-MS. Erlotinib is a tyrosine kinase inhibitor that acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC₅₀ = 2.5 μM). This inhibits tumor growth in human head and neck carcinoma (HN5) tumor xenografts in mice with an ED₅₀ value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC₅₀ = 4.6 μM) and JAK2 mutant JAK2^V617F (IC₅₀ = 5 μM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia. Formulations containing erlotinib are used to treat certain forms of cancer, including non-small cell lung cancer.