LY3039478 Crenigacestat

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Chemical Information

Product name：LY3039478 Crenigacestat	Purity：99% min
CAS NO：1421438-81-4	Solubility：DMSO : ≥ 34 mg/mL (73.21 mM)
Molecular Formula：C₂₂H₂₃F₃N₄O₄	Package：Package according to customer requirements.
Molecular Weight：464.438	Storage：Store at -20℃

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Remarks

Crenigacestat, also known as LY3039478, is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. LY3039478 potently inhibits mutant Notch receptor activity. In a xenograft tumor model, LY3039478 inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment. LY3039478 is being investigated in Phase I.

Gamma-secretase Inhibitors Related Products:

RO4929097; Semagacestat; Avagacestat; Dibenzazepine; LY-411575; DAPT (GSI-IX)

References

[1]. Yuen E, et al. Evaluation of the effects of an oral notch inhibitor, crenigacestat (LY3039478), on QT interval, and bioavailability studies conducted in healthy subjects. Cancer Chemother Pharmacol. 2019 Mar;83(3):483-492.

[2]. 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.