Lapatinib Ditosylate

Lapatinib Ditosylate               
            上海义森生物科技有限公司技术数据:

分子量(MW):	925.46
化学式:	C29H26ClFN4O4S.2C7H8O3S
溶解度:	DMSO 185mg/mL   Water <1mg/mL   Ethanol <1mg/mL
纯度:	99%
稳定性:	at -20℃ 2 years
CAS号:	388082-77-7, 231277-92-2 (free base), 1187538-35-7 (4-methylbenzenesulfonate)

生物活性Lapatinib Ditosylate (Tykerb) was found to have 50% inhibitory concentration (IC50) values against purified EGFR and HER2 of 10.2 and 9.8 nM, respectively. And IC50 >10000nM against c-Raf-1,MEK,ERK,CDK1CDK2,p38 and VEGFR-2.
The IC50s for inhibition of cell growth by 72h treatment with GW2016 are 0.16μM for A431,0.12 μM for HN5,0.10 μM for BT474,0.09 μM for N87.
Lapatinib undergoes first-pass metabolism catalyzed by CYP3A4/5 and does not appear to be a substrate for P-glycoprotein. [2]