Desmethyl Erlotinib

Desmethyl Erlotinib

CAT N°: 23394
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From 102.00 86.70

Desmethyl erlotinib is a metabolite of erlotinib (Item No. 10483).{40416} Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM).{18354,18362} This inhibits tumor growth in human head and neck carcinoma HN5 tumor xenografts in mice with an ED50 value of 9 mg/kg.{18354} Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 µM) and JAK2 mutant JAK2V617F positive hematopoietic progenitor cells (IC50 = 5 µM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia.{16061,18355} Formulations containing erlotinib have been used to treat certain forms of cancer, including non-small cell lung cancer.{18351,17857}

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