Crenigacestat

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].

Product Specifications

CAS Number

[1421438-81-4]

Product Name Alternative

LY3039478

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Notch; γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/LY3039478.html

Concentration

10mM

Purity

99.01

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(N[C@@H](C)C(N[C@H]1C2=CC=CC=C2C3=CC=CN=C3N(CCO)C1=O)=O)CCC(F)(F)F

Molecular Formula

C22H23F3N4O4

Molecular Weight

464.44

Precautions

H302, H315, H319, H335

References & Citations

[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.