产品信息
抗原名称
γ secretase(Aβ42),γ secretase(Aβ40)
商品描述
BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.
分子量
520.88
纯度
>98%
可溶性
DMSO : 96 mg/mL (184.3 mM)
外观
Powder
In vitro(体外研究)
BMS-708163 exhibits weaker potency for inhibition of Notch processing, IC50=58±23 nM, as compared to its inhibition potency for APP cleavage. BMS-708163 (10 µM) combined with gefitinib significantly attenuates the colony growth of PC9/AB2 cells, increases the expression of active caspase 3 and PARP and reduces the expression of Ki-67 in PC9/AB2 cells. BMS-708163 induces apoptosis and enhances cell cycle arrest at the G1 phase in PC9/AB2 cells. BMS-708163 treatment effectively downregulates the expression of Notch1, HES1, PI3K and Akt in PC9/AB2 cells.
In vivo(体内研究)
BMS-708163 significantly reduces both plasma and brain Aβ40 levels relative to control at 10 and 100 mg/kg for the entire dosing interval, demonstrates significant Aβ40 lowering for 8 h after an oral dose of 1 mg/kg, and significantly lowers CSF Aβ40 levels in rats, when measured 5 h after single oral doses ranging from 3 to 100 mg/kg. BMS-708163 (10 mg/kg) monotherapy has a minor inhibitory effect on PC9/AB2 tumor growth compared with gefitinib alone. BMS-708163 monotherapy results in a slight increase in caspase 3 expression as well as a mild decrease in Ki-67 expression in vivo. In the xenograft lung cancer samples treated with BMS-708163 plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining.
背景
别名
BMS708163；BMS 708163；Avagacestat
分子式
C20H17ClF4N4O4S
CAS号
1146699-66-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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