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  3. CZ415

CZ415 

Cat. No.: HY-100222 Purity: 98.43%
Handling Instructions

CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

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

CZ415 Chemical Structure

CZ415 Chemical Structure

CAS No. : 1429639-50-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 888 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CZ415 purchased from MCE. Usage Cited in: Oncotarget. 2017 May 30;8(47):82027-82036.

    U0126 and MEK162 block ERK activation (p-ERK1/2) in CZ415-treated U2OS cells.

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    • Customer Review

    Description

    CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

    IC50 & Target[1]

    mTOR

    8.07 (pIC50)

    mTORC1

     

    mTORC2

     

    In Vitro

    Inhibition of phosphorylation for both downstream targets results in 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT. The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 hours in stimulated human whole blood and the resulting IC50 is 226 nM. As a predictor for cardiotoxicity, the activity of CZ415 against the human cardiac ion channel hERG is assessed in a whole-cell patch-clamp assay in HEK293 cells resulting in an IC50 of 48 μM[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    CZ415 is a highly selective mTOR inhibitor showing in vivo efficacy in a collagen induced arthritis (CIA) model. For full characterization of CZ415 and to enable improved dose predictions, the pharmacokinetic (PK) profile is assessed in rat. PK and oral bioavailability are determined after of 1 mg/kg intravenous (iv) bolus and 3 mg/kg oral (po) administration. The observed plasma clearance, corresponding to 45% liver blood flow, suggests that sufficient levels of free compound are circulating in the animal over time. The oral uptake is rapid with a Tmaxmax of 0.5 h and bioavailability F = 44% indicates very good absorption from the gut[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    459.56

    Formula

    C₂₂H₂₉N₅O₄S

    CAS No.

    1429639-50-8

    SMILES

    O=C(NCC)NC(C=C1)=CC=C1C2=NC3=C(CS(C3(C)C)(=O)=O)C(N4[[email protected]@H](C)COCC4)=N2

    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 : 100 mg/mL (217.60 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1760 mL 10.8800 mL 21.7599 mL
    5 mM 0.4352 mL 2.1760 mL 4.3520 mL
    10 mM 0.2176 mL 1.0880 mL 2.1760 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 (5.44 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    Mice[1]
    To determine the effects of CZ415 on its pharmacological target, dose-dependent changes in phosphorylation levels of S6 Ribosomal Protein and Akt - both downstream targets of mTOR are assessed. CZ415 is administered orally at 1, 3 and 10 mg/kg to mice 1 h before anti-CD3 stimulus. 15 min after stimulation, spleens are dissected and analyzed for pS6RP and pAKT levels. A dose related significant inhibition of phosphorylation of both S6RP and Akt are observed after compound administration. In particular, 1 and 3 mg/kg CZ415 could fully inhibit S6RP phosphorylation induced by anti-CD3 stimulation and 10 mg/kg additionally decreased the constitutive phosphorylation levels as measured in the control group.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    CZ415CZ 415CZ-415mTORMammalian target of RapamycinInhibitorinhibitorinhibit

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