857876-30-3

溶解度:Soluble in DMSO at 200 mg/ml

储存条件:-20C 2 years

生物活性

Lapatinib is a potent inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM), ErbB-4 kinase (Ki = 347 nM). Lapatinib can restore tamoxifen sensitivity in tamoxifen-resistant, ER-positive breast cancer models.

参考文献

1��Burris, H.A. III "Dual Kinase Inhibition in the Treatment of Breast Cancer: Initial Experience with the EGFR/ErbB-2 Inhibitor Lapatinib." Oncologist 9: 10-15 (2004).

2��Wood, E.R., et al. "A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib), Relationships among Protein Conformation, Inhibitor Off-Rate, and Receptor Activity in Tumor Cells." Cancer Res. 64: 6652-6659 (2004).