Lapatinib-d<sub>4</sub> (tosylate)

Lapatinib-d4 (tosylate)

CAT N°: 25459
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From 420.00 357.00

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 ?M, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 ?M, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 ?M).{36874} It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 ?M. 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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