Product Description: Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested[1][2][3][4].
Applications: Cancer-programmed cell death
Formula: C22H23F3N4O4
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./[3]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./[4]Mark H. Bender, et al. Abstract 1131: Novel inhibitor of Notch signaling for the treatment of cancer. Experimental and Molecular Therapeutics. 2013.
CAS Number: 1421438-81-4
Molecular Weight: 464.44
Compound Purity: 99.01
Research Area: Cancer
Solubility: DMSO : ≥ 34 mg/mL
Target: Notch;γ-secretase
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