Lapatinib

  • Chemical Properties
CAS No. 231277-92-2 Cat. No. BCP01874
Name Lapatinib
Synonyms GSK572016; GSK-572016; GSK 572016; GW2016; GW-2016; GW 2016;
Formula C29H26ClFN4O4S M. Wt 581.06
  • Biological Activity
Description Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells.
Related Products 388082-78-8(Lapatinib Ditosylate) 388082-77-7(Lapatinib ditosylate)
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway 
Targets EGFR HER2 

Structure

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