Description
Erlotinib-d
6 (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 (IC
50 = 2.5 μM). This inhibits tumor growth in human head and neck carcinoma (HN5) tumor xenografts in mice with an ED
50 value of 9 mg/kg. Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC
50 = 4.6 μM) and JAK2 mutant JAK2
V617F (IC
50 = 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.
Uses
Erlotinib D6 HCl is a Selective epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor, Antineoplastic.;Labeled Erlotinib, intended for use as an internal standard for the quantification of Erlotinib by GC- or LC-mass spectrometry.
