Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl-d4]amino]methyl]-2-furanyl]-4-quinazolinamine, 4-methylbenzenesulfonate (1:2)
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C29H22ClD4FN4O4S / 2C7H8O3S
Formula Weight: 929.487883
CAS Number: 2749856-05-9
Notes: Lapatinib-d4 is intended for use as an internal standard for the quantification of lapatinib (Item No. 11493) by GC- or LC-MS. Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively).{24151} It inhibits the growth of EGFR-overexpressing A431 skin cancer and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50s = 0.14 and 0.124 μM, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 μM, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 μM).{36874} It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 μM. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model.{36875} It also reduces tumor growth in an NCI-N87 mouse xenograft model when administered at a dose of 100 mg/kg and induces tumor regression when used in combination with trastuzumab.{36874} Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of ErbB2/HER2-overexpressing breast cancer.
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