1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. CAY10566

CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).

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

CAS No. : 944808-88-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 18 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119.  [Abstract]

    XBP1 splicing in OVCAR-5 cells cultured in low-serum conditions and treated with SCD inhibitor CAY10566 (0-24.3 nM) for 48 h.

    CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119.  [Abstract]

    XBP1 splicing in primary cells from tumors of OC patients cultured in low-serum conditions and treated with 3 μM CAY10566 for 48 h or with 1 μM CAY10566 and 50 μM PA for 12 h.

    CAY10566 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Oct 11;119(41):e2203480119.  [Abstract]

    XBP1 splicing in OVCAR-5 cells cultured in medium containing low serum and treated with 21.6 nM CAY10566 and indicated doses of OA for 48 h.

    CAY10566 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Jan;38:101807.  [Abstract]

    FBW7 silencing PANC-1 and SW1990 cells were treated with RSL3 (2 μmol/L) or CAY10566 (5 μmol/L) for 48–72 h and then detected cell viability.

    CAY10566 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Jan;38:101807.  [Abstract]

    TEM imaging was conducted in FBW7T205A overexpressed PANC-1 cells. RSL3 (2 μmol/L) and CAY10566 (5 μmol/L) treated PANC-1 cells functioned as the positive control. Red arrows showed the shrunken mitochondria. Blue arrows showed lipid droplets. The values below the western blot band represent the relative mean gray values of three independent experiments. Gray values were calculated by Adobe Photoshop CS6.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM)[1][2].

    IC50 & Target

    IC50: 4.5 nM (SCD1 in mouse), 26 nM (SCD1 in human)[2]

    Cellular Effect
    Cell Line Type Value Description References
    NCI-H1155 IC50
    < 10 nM
    Compound: 4
    Inhibition of SCD in human NCI-H1155 cells non-expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
    Inhibition of SCD in human NCI-H1155 cells non-expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
    [PMID: 32787093]
    NCI-H2122 IC50
    < 10 nM
    Compound: 4
    Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
    Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
    [PMID: 32787093]
    In Vitro

    CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation[3].

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

    Cell Proliferation Assay[3]

    Cell Line: Swiss 3T3 cells
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 24 hours
    Result: Swiss 3T3 cell proliferation was concentration-dependently decreased.
    In Vivo

    After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[4].

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

    Molecular Weight

    389.81

    Formula

    C18H17ClFN5O2

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 25 mg/mL (64.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Acetone : 10 mg/mL (25.65 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5654 mL 12.8268 mL 25.6535 mL
    5 mM 0.5131 mL 2.5654 mL 5.1307 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.93%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Acetone / DMSO 1 mM 2.5654 mL 12.8268 mL 25.6535 mL 64.1338 mL
    5 mM 0.5131 mL 2.5654 mL 5.1307 mL 12.8268 mL
    10 mM 0.2565 mL 1.2827 mL 2.5654 mL 6.4134 mL
    15 mM 0.1710 mL 0.8551 mL 1.7102 mL 4.2756 mL
    20 mM 0.1283 mL 0.6413 mL 1.2827 mL 3.2067 mL
    25 mM 0.1026 mL 0.5131 mL 1.0261 mL 2.5654 mL
    DMSO 30 mM 0.0855 mL 0.4276 mL 0.8551 mL 2.1378 mL
    40 mM 0.0641 mL 0.3207 mL 0.6413 mL 1.6033 mL
    50 mM 0.0513 mL 0.2565 mL 0.5131 mL 1.2827 mL
    60 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0689 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
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    Cat. No.:
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