Lapatinib ditosylate monohydrate 是一种有效的 EGFR 和 ErbB2 抑制剂，对EGFR和ErbB2的IC50值分别为 10.8 和 9.2 nM。它用于治疗晚期乳腺癌和其他实体瘤。

Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.

In vitro kinase assays: The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.

388082-78-8

C43H44ClFN4O11S3

943.47

Lapatinib tosilate;Lapatinib ditosylate monohydrate;Lapatinib ditoluenesulfonate monohydrate;Tyverb;Tykerb;二甲苯磺酸拉帕替尼单水合物;Lapatinib tosilate hydrate

DMSO:91 mg/mL(96.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years