產品名稱：Lapatinib, Di-p-Toluenesulfonate Salt
產品貨號：LC  L-4804 
產品規格：1 MG
Lapatinib inhibits both epidermal growth factor receptor (EGFR) and HER2/neu (ErbB-2) tyrosine kinases by binding to the intracellular phosphorylation domain, preventing receptor autophosphorylation.  The exact site of binding has currently not been confirmed.  It appears to arrest the development of breast cancer in some patients with metastatic, treatment-refractory disease.  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).
Potent inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM), ErbB-4 kinase (Ki = 347 nM).  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).
Lapatinib can restore tamoxifen sensitivity in tamoxifen-resistant, ER-positive breast cancer models.  Chu, I., et al. "The Dual ErbB1/ErbB2 Inhibitor, Lapatinib (GW572016), Cooperates with Tamoxifen to Inhibit Both Cell Proliferation- and Estrogen-Dependent Gene Expression in Antiestrogen-Resistant Breast Cancer."  Cancer Res. 65:  18-25 (2005).
Lapatinib ditosylate is the active ingredient in the drug sold under the trade names Tykerb® in the US and Tyverb in Europe.  This drug has been approved in at least one country to treat advanced metastatic breast cancer in conjunction with the chemotherapy drug Xeloda.  NOTE:  The lapatinib ditosylate sold by LC Laboratories is NOT Tykerb® or Tyverb, and is NOT for human use.
The CAS number for the free base of lapatinib is [231277-92-2].
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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