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L-4804 Lapatinib, Di-p-Toluenesulfonate Salt, >98%

[Lapatinib Ditosylate] [Tykerb] [GW-572016] [Tyverb]

M.W. 925.48

C29H26ClFN4O4S•2C7H8O3S

[388082-78-8]

M.I. 14:  5367

Storage:  Store at or below -20 ºC.  Solubility:  Slightly soluble in DMSO.  Disposal:  A

View the MSDS for this product

• 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 regenerate 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 is approved to treat advanced metastatic breast cancer in conjunction with the chemotherapy drug Xelod.

• The CAS number for the free base of lapatinib is [231277-92-2].

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Section 68B of the Patents Act of 1953 in New Zealand; (vi) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (vii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.