Lapatinib, Free Base
N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine, GSK 572016, GW-572016, GW 572016X, Tykerb, Tyverb
ATP-competitive EGFR & ErbB-2 dual tyrosine kinase inhibitor. Lapatinib is an ATP-competitive epidermal growth factor receptor (EGFR) and HER2/neu (ErbB-2) dual tyrosine kinase inhibitor, with IC(50) values of 10.8 and 9.2nm respectively. It is an orally active drug for treatment of breast cancer and other solid tumors. A free base form of Lapatinib Ditosylate. Lapatinib (as the 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 (generic name, capecitabine).
Solubility
Soluble 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.
Melting Point: As Reported
Storage and Stability
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Form
Supplied as a pale yellow powder.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
