Crenigacestat (LY3039478, LY-3039478)是可口服的、有效的Notch和γ-secretase的抑制剂，对Notch的IC₅₀值为0.41 nM，具有抗肿瘤活性，目前在临床开发阶段。LY3039478是Notch-1胞内结构域(N1ICD)切割活性的抑制剂，在多种肿瘤细胞中IC₅₀为1 nM，抑制Notch下游调控基因表达。

参考文献

1.Mäemets-Allas K, et al. The inhibition of Akt-Pdpk1 interaction efficiently suppresses the growth of murine primary liver tumor cells. Biochem Biophys Res Commun. 2016 May 20;474(1):118-125.

2.Bhagat TD, et al. Notch Pathway Is Activated via Genetic and Epigenetic Alterations and Is a Therapeutic Target in Clear Cell Renal Cancer. J Biol Chem. 2017 Jan 20;292(3):837-846.

3.Mark H. Bender, et al. Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer. Cancer Res. 2013.

冰袋运输。粉末直接保存于-20℃，有效期3年。建议分装后-20℃干燥保存，避免反复冻融。