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

SAR405 

Cat. No.: HY-12481 Purity: 99.94%
Handling Instructions

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.

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

SAR405 Chemical Structure

SAR405 Chemical Structure

CAS No. : 1523406-39-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 127 In-stock
Estimated Time of Arrival: December 31
2 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
Estimated Time of Arrival: December 31
25 mg USD 460 In-stock
Estimated Time of Arrival: December 31
50 mg USD 790 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of SAR405:

Top Publications Citing Use of Products

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

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

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

    Serum-starved H4IIEC3 cells are treated with 100 nM insulin (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.
    • Biological Activity

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    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

     

    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].

    Molecular Weight

    443.85

    Formula

    C₁₉H₂₁ClF₃N₅O₂

    CAS No.

    1523406-39-4

    SMILES

    O=C1N(C2=NC(N3[[email protected]](C)COCC3)=C1)CC[[email protected]@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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 27 mg/mL (60.83 mM)

    *"≥" 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
    10 mM 0.2253 mL 1.1265 mL 2.2530 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 (5.63 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

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

    Purity: 99.94%

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