Fosamprenavir Calcium Salt 是抗逆转录病毒蛋白酶抑制剂 Amprenavir 的磷酸酯前药,具有改善的溶解性和抗HIV感染作用。
产品描述
Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Fosamprenavir Calcium Salt has Anti-HIV infection.
体内活性
Oral gavage of DATS significantly retarded growth of PC-3 xenografts in athymic mice without causing weight loss. For instance, 20 days after starting therapy, the average tumor volume in control mice was approximately 3-fold higher compared with DATS-treated mice. Tumors from DATS-treated mice exhibited a markedly higher count of apoptotic bodies compared with control tumors. Consistent with the results in cultured PC-3 cells, the DATS-mediated suppression of PC-3 xenograft growth correlated with induction of proapoptotic proteins Bax and Bak. Although DATS treatment inhibited migration of cultured PC-3 cells in association with down-regulation of vascular endothelial growth factor receptor-2 protein, formation of new blood vessels was comparable in tumors of control and DATS-treated mice as judged by CD31 immunostaining[1].
动物实验
DATS was given orally (6 micromoL, thrice weekly) to male athymic mice s.c. implanted with PC-3 cells. Tumor sections from control and DATS-treated mice were examined for apoptotic bodies by terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling assay. Protein levels of apoptosis and cell cycle regulating proteins in tumor tissues of control and DATS-treated mice were determined by immunoblotting. The effect of DATS treatment on in vivo angiogenesis was determined by immunohistochemical analysis of CD31 in tumors[1].
Cas No.
226700-81-8
分子式
C25H34CaN3O9PS
分子量
623.67
别名
福沙那伟钙;GW433908G
储存和溶解度
DMSO:1.8 mg/mL (2.89 mM),Need ultrasonic and warming
H2O:0.25 mg/mL (0.40 mM),Need ultrasonic and warming
DMSO:5mg/ml(28.04mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years