Lapatinib, Di-p-Toluenesulfonate Salt (N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine Ditosylate, Lapatinib Ditosylate, Tykerb, GW-572016, Tyverb)

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.\n\nSolubility:\nSoluble in DMSO at 200mg/ml; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-10uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.\n\nElemental Anaylsis:\nCalculated: \nC=54.22%\nH=4.76%\nCl=3.72%\nF= 1.99%\nN=5.88%\nS= 10.10%\n\nStorage and Stability:\nLyophilized powder may be stored at -20 degrees C. Stable for 6 months.

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SPECIFICATIONS

Catalog Number

L1315-50

Size

100mg

Form

Supplied as a yellow powder.

Purity

~99%

References

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). 3. 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).