2. PI3K/Akt/mTOR
  3. PI3K
  4. PI-3065

PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

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

PI-3065 Chemical Structure

PI-3065 Chemical Structure

CAS No. : 955977-50-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 100 In-stock
Solution
10 mM * 1 mL in DMSO USD 100 In-stock
Solid
1 mg USD 36 In-stock
5 mg USD 90 In-stock
10 mg USD 145 In-stock
25 mg USD 260 In-stock
50 mg USD 420 In-stock
100 mg USD 695 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

PI-3065 Related Antibodies

Top Publications Citing Use of Products

    PI-3065 purchased from MedChemExpress. Usage Cited in: Cell Signal. 2016 Mar;28(3):148-56.  [Abstract]

    Inhibition of PI3K p110δ signalling, either by PI3KCD-/- or using PI3K p110δ inhibitor PI-3065, significantly blocks LPS-induced GSK3α phosphorylation.

    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

    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.

    IC50 & Target[1]

    p110δ

    5 nM (IC50)

    p110β

    600 nM (IC50)

    p110α

    910 nM (IC50)

    In Vitro

    PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ[1].

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

    PI-3065 Related Antibodies
    In Vivo

    PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss[1].

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

    506.64

    Formula

    C27H31FN6OS
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC(C=CC1=C2C=CN1)=C2C3=NC4=C(SC(CN5CCN(CC6CC6)CC5)=C4)C(N7CCOCC7)=N3
    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 : 25 mg/mL (49.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9738 mL 9.8689 mL 19.7379 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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 (4.93 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.93 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)

    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: 98.97%

    COA (249 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×105 4T1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12 h prior to tumour cell inoculation). Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescence measurement, followed by fixation in 4% PFA and H&E staining. KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of 14 days.

    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 1.9738 mL 9.8689 mL 19.7379 mL 49.3447 mL
    5 mM 0.3948 mL 1.9738 mL 3.9476 mL 9.8689 mL
    10 mM 0.1974 mL 0.9869 mL 1.9738 mL 4.9345 mL
    15 mM 0.1316 mL 0.6579 mL 1.3159 mL 3.2896 mL
    20 mM 0.0987 mL 0.4934 mL 0.9869 mL 2.4672 mL
    25 mM 0.0790 mL 0.3948 mL 0.7895 mL 1.9738 mL
    30 mM 0.0658 mL 0.3290 mL 0.6579 mL 1.6448 mL
    40 mM 0.0493 mL 0.2467 mL 0.4934 mL 1.2336 mL
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    PI-3065 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:

    PI-3065955977-50-1PI3065PI 3065PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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