A Notch inhibitor
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Crenigacestat

Item No. 27919

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-[[(7S)-6,7-dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido[3,2-a][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]-4,4,4-trifluoro-butanamide
CAS Number
1421438-81-4
Synonyms
  • LY3039478
Molecular Formula
C22H23F3N4O4
Formula Weight
464.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 0.5 mg/ml
λmax
227 nm
SMILES
O=C1[C@@H](NC([C@H](C)NC(CCC(F)(F)F)=O)=O)C2=CC=CC=C2C3=C(N=CC=C3)N1CCO
InChi Code
InChI=1S/C22H23F3N4O4/c1-13(27-17(31)8-9-22(23,24)25)20(32)28-18-15-6-3-2-5-14(15)16-7-4-10-26-19(16)29(11-12-30)21(18)33/h2-7,10,13,18,30H,8-9,11-12H2,1H3,(H,27,31)(H,28,32)/t13-,18-/m0/s1
InChi Key
YCBAQKQAINQRFW-UGSOOPFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $223

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    10 mg

    $423

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    Cayman Chemical
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    Product Description

    Crenigacestat is an orally bioavailable Notch inhibitor.1 It induces cell cycle arrest at the G0/G1 phase and decreases expression of the oncogenes MYC and CCNA1 in Caki human renal cancer cells.2 Crenigacestat (8 mg/kg per day) reduces tumor growth and increases survival in a 769-P mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yuen, E., Posada, M., Smith, C., 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. 83(3), 483-492 (2019).

    2. Bhagat, T.D., Zou, Y., Huang, S., et al. Notch pathway is activated via genetic and epigenetic alterations and is a therapeutic target in clear cell renal cancer. The Journal of Biological Chemisty 292(3), 837-846 (2017).