1. Neuronal Signaling
    Stem Cell/Wnt
  2. Notch
    γ-secretase
  3. Crenigacestat

Crenigacestat (Synonyms: LY3039478)

Cat. No.: HY-12449 Purity: 98.62%
Handling Instructions

Crenigacestat is an orally active Notch and γ-secretase inhibitor, with an IC50 of ∼1nM in most of the tumor cell lines tested.

For research use only. We do not sell to patients.

Crenigacestat Chemical Structure

Crenigacestat Chemical Structure

CAS No. : 1421438-81-4

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10 mM * 1  mL in DMSO USD 172 In-stock
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10 mg USD 264 In-stock
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25 mg USD 528 In-stock
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50 mg USD 840 In-stock
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100 mg USD 1320 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Crenigacestat purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Oct 28. 

    The Western blot analysis results show that LY3039478 inhibits not only Notch1 but also APRIL.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Crenigacestat is an orally active Notch and γ-secretase inhibitor, with an IC50 of ∼1nM in most of the tumor cell lines tested[1][2][3][4].

    In Vitro

    Crenigacestat (100 nM) exhibits anti-cancer activity in K07074 cells (a primary mouse liver tumor cell line)[2].
    Crenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells[3].

    Cell Viability Assay[2].

    Cell Line: K07074 cells.
    Concentration: 100 nM.
    Incubation Time: 24-96 hours.
    Result: Effectively reduced the growth of K07074 cells.
    In Vivo

    Crenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC[3].

    Animal Model: CCRCC xenografts were established in NOD-scid IL2R null mice with subcutaneous implantation using the 769-P cell line[3].
    Dosage: 8 mg/kg.
    Administration: Oral gavage three times a week.
    Result: Resulted in increased overall survival when compared with vehicle control in CCRCC xenografts.
    Clinical Trial
    Molecular Weight

    464.44

    Formula

    C₂₂H₂₃F₃N₄O₄

    CAS No.

    1421438-81-4

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 34 mg/mL (73.21 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1531 mL 10.7657 mL 21.5313 mL
    5 mM 0.4306 mL 2.1531 mL 4.3063 mL
    10 mM 0.2153 mL 1.0766 mL 2.1531 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 98.62%

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    Keywords:

    CrenigacestatLY3039478LY 3039478LY-3039478Notchγ-secretaseGamma secretaseliverCCRCCInhibitorinhibitorinhibit

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