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Avagacestat

CAS No. : 1146699-66-2

MCE 国际站：Avagacestat

产品活性：Avagacestat (BMS-708163) 是有效的 γ-secretase 抑制剂，抑制 Aβ42 和 Aβ40 的产生，IC₅₀ 值分别为 0.27 nM 和 0.30 nM；BMS-708163 同时抑制 Notch 胞内结构域 (NICD) 和 CYP2C19，IC₅₀ 值分别为 0.84 nM 和 20 μM。Avagacestat 可用于阿尔兹海默症的研究。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase  |  Notch

In Vitro: Avagacestat (BMS-708163) exhibits weaker potency for inhibition of Notch processing, IC₅₀=58±23 nM, as compared to its inhibition potency for APP cleavage. Avagacestat (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. Avagacestat (BMS-708163) induces apoptosis and enhances cell cycle arrest at the G1 phase in PC9/AB2 cells. Avagacestat (BMS-708163) treatment effectively downregulates the expression of Notch1, HES1, PI3K and Akt in PC9/AB2 cells.

In Vivo: Avagacestat (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. Avagacestat (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 Avagacestat (BMS-708163) plus gefitinib, there are a marked increase in caspase 3 expression and a reduction in Ki-67 staining.

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