L-4804 Lapatinib, Di-p-Toluenesulfonate Salt, >99%

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.

BLP-112 BLP-111 BLP-110 BLP-109 BLP-108 BLP-107 BLP-106 BLP-105 BLP-104 BLP-103 BLP-102 BLP-101

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• More than 720 labs worldwide have purchased Lapatinib or its salt forms from LC Labs (either directly from us or from our many distributors, many of whom resell under their own labels).
• This research compound is the di-p-toluenesulfonate salt form of Lapatinib.  Please see the free base form of lapatinib, Cat. No. L-4899, Lapatinib, Free Base, for further technical information.
• This lapatinib product is the di-p-toluenesulfonate Salt, whose CAS number is given above.  The CAS number of the  free base form of lapatinib is 231277-92-2.
• 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 Di-p-Toluenesulfonate Salt 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 SOLD BY LC LABORATORIES FOR RESEARCH IS NOT TYKERB® OR TYVERB®, AND IS NOT FOR HUMAN USE.
• 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) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) 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.