2. PI3K/Akt/mTOR Autophagy
  3. PI3K Autophagy
  4. SAR405

SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

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SAR405 Chemical Structure

SAR405 Chemical Structure

CAS No. : 1523406-39-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of SAR405:

SAR405 Related Antibodies

Top Publications Citing Use of Products

    SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805.  [Abstract]

    Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min and electrophoresed protein extracts subjected to western blotting using antibodies against total or phosphorylated p42/p44 MAPK.

    SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805.  [Abstract]

    Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min, and electrophoresed protein extracts subjected to western blotting using antibodies against pAktS473 and Akt.

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity[1][2].

    IC50 & Target[1]

    Vps34

    1.2 nM (IC50)

    Vps34

    1.5 nM (Kd)

    Autophagy

     

    Cellular Effect
    Cell Line Type Value Description References
    Cortical neurone EC50
    2.4 μM
    Compound: SAR405
    Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay
    Neuroprotective activity in rat cortical neurons transfected with an mHTT-exon1-Q73 construct in presence of primary corticostriatal co-culture system assessed as rescue from mHTT-induced survival loss by fluorescent reporter based assay
    		[PMID: 30840447]
    In Vitro

    The activity of SAR405 is next evaluated on a dedicated Vps34 cellular assay using a GFP-FYVE–transfected HeLa cell line[1].
    SAR405 prevents autophagy and synergizes with mTOR inhibition in tumor cells. SAR405 prevents autophagosome formation with an IC50 of 42 nM. Treatment of starved cells with SAR405 completely inhibits the conversion to LC3-II in a dose-dependent manner. The effect of SAR405 on autophagy is then investigated. The GFP-LC3 model is used for the HTS and confirmed its activity on starved cells (IC50=419 nM). The conversion of LC3-I into LC3-II is also analyzed by western blotting on wild-type HeLa and H1299 cells[2].

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

    SAR405 Related Antibodies
    Molecular Weight

    443.85

    Formula

    C19H21ClF3N5O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C1N(C2=NC(N3[C@H](C)COCC3)=C1)CC[C@@H](C(F)(F)F)N2CC4=CC(Cl)=CN=C4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 27 mg/mL (60.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2530 mL 11.2651 mL 22.5301 mL
    5 mM 0.4506 mL 2.2530 mL 4.5060 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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

    ×
    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.63 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.63 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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: 99.74%

    SDS (393 KB)

    COA (253 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    KiNativ profiling is performed. Jurkat cell lysates are treated with 1 μM of SAR405. After 15-min incubation, the desthiobiotin-ATP-acylphosphate probe is added and incubated for 10 min. Samples are prepared for targeted MS analysis. Briefly, samples are prepared for trypsin digestion (denature and then reduce alkylate) and digested with trypsin, and desthiobiotinylated peptides are enriched on streptavidin resin. Enriched probe-labeled peptides are analyzed by LC tandem MS on a Thermo-LTQ ion trap mass spectrometer using proprietary data collection methodology. All quantification is performed by extracting characteristic fragment ion signals from targeted MS/MS spectra and comparing signals in control and treated samples[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2530 mL 11.2651 mL 22.5301 mL 56.3253 mL
    5 mM 0.4506 mL 2.2530 mL 4.5060 mL 11.2651 mL
    10 mM 0.2253 mL 1.1265 mL 2.2530 mL 5.6325 mL
    15 mM 0.1502 mL 0.7510 mL 1.5020 mL 3.7550 mL
    20 mM 0.1127 mL 0.5633 mL 1.1265 mL 2.8163 mL
    25 mM 0.0901 mL 0.4506 mL 0.9012 mL 2.2530 mL
    30 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8775 mL
    40 mM 0.0563 mL 0.2816 mL 0.5633 mL 1.4081 mL
    50 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1265 mL
    60 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
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    SAR405 Related Classifications

    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.

    Keywords:

    SAR4051523406-39-4SAR 405SAR-405PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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