Avagacestat (BMS-708163, BMS708163)，也称塞来西布，是具有口服活性的选择性γ-分泌酶(γ-secretase)抑制剂，抑制Aβ40和Aβ42产生，IC₅₀分别为0.3 nM和0.27 nM，Aβ在细胞基质聚积后具有很强的神经毒性作用。Avagacestat作用于Notch表现出低选择性，但效果好于LY450139，Avagacestat在临床上大剂量给药会导致Notch水解产生抑制进而表现出毒性。Avagacestat也抑制人重组CYP同工酶，IC₅₀为20 μM。

参考文献

1. Gillman KW, et al. Letter Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4.
2. Crump CJ, et al. BMS-708,163 targets presenilin and lacks notch-sparing activity. Biochemistry. 2012 Sep 18;51(37):7209-11.
3. Xie M, et al. γ Secretase inhibitor BMS-708163 reverses resistance to EGFR inhibitor via the PI3K/Akt pathway in lung cancer. J Cell Biochem. 2015 Jun;116(6):1019-27.
4. Borghys H, et al. A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators. J Alzheimers Dis. 2012;28(4):809-22.

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