Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy-1,1,2,2,3,3-d6]-4-quinazolinamine
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C22H18ClD6FN4O3
Formula Weight: 452.9
CAS Number: 1228664-49-0
Notes: Gefitinib-d6 is intended for use as an internal standard for the quantification of gefitinib (Item No. 13166) by GC- or LC-MS. Gefitinib is an EGFR inhibitor (IC50s = 0.023-0.079 µM).{61750} It inhibits colony formation of GEO colon, ZR-75-1 and MCF-10A breast, and OVCAR-3 ovarian cancer cell lines in soft agar assays (IC50s = 0.2-0.4 µM).{17856} Gefitinib (0.1 to 1 µM) induces apoptosis and inhibits EGFR autophosphorylation in the same cells. In vivo, gefitinib (1.25, 2.5, and 5 mg/kg) reduces tumor volume and increases survival in a GEO mouse xenograft model. Formulations containing gefitinib have been used in the treatment of non-small cell lung cancer (NSCLC).