1. PI3K/Akt/mTOR
  2. PI3K
  3. PI3K-IN-1

PI3K-IN-1  (Synonyms: XL-147 derivative 1)

Cat. No.: HY-12068 Purity: 96.02%
COA Handling Instructions

PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.

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

PI3K-IN-1 Chemical Structure

PI3K-IN-1 Chemical Structure

CAS No. : 1349796-36-6

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 117 In-stock
Solution
10 mM * 1 mL in DMSO USD 117 In-stock
Solid
2 mg USD 55 In-stock
5 mg USD 88 In-stock
10 mg USD 154 In-stock
25 mg USD 308 In-stock
50 mg USD 440 In-stock
100 mg USD 715 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PI3K-IN-1 purchased from MedChemExpress. Usage Cited in: Front Bioeng Biotechnol. 2020 May 8;8:392.  [Abstract]

    Acta2 expression after Signaling inhibitors by q-PCR. For inhibitor treatment, 24 h after seeding, the medium is removed and replaced with the PI3K inhibitor PI3K-IN-1(25 μM) to block the PI3K/Akt signaling pathways.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways[1].

    IC50 & Target[1]

    PI3K

     

    In Vitro

    PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways. By using the PI3K inhibitor PI3K-IN-1, TGF-β1 induced transformation into myofibroblast is also inhibited, with relatively reduced expressions of α-SMA, Col-1 and Timp-1[1].

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

    Molecular Weight

    599.66

    Formula

    C31H29N5O6S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    COC1=CC(NC2=NC3=CC=CC=C3N=C2NS(C4=CC=C(C=C4)NC(C5=CC=C(C(OC)=C5)C)=O)(=O)=O)=CC(OC)=C1

    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 : 27.5 mg/mL (45.86 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6676 mL 8.3381 mL 16.6761 mL
    5 mM 0.3335 mL 1.6676 mL 3.3352 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
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    Volume
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    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 (4.17 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 (4.17 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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: 99.93%

    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, 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 1.6676 mL 8.3381 mL 16.6761 mL 41.6903 mL
    5 mM 0.3335 mL 1.6676 mL 3.3352 mL 8.3381 mL
    10 mM 0.1668 mL 0.8338 mL 1.6676 mL 4.1690 mL
    15 mM 0.1112 mL 0.5559 mL 1.1117 mL 2.7794 mL
    20 mM 0.0834 mL 0.4169 mL 0.8338 mL 2.0845 mL
    25 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6676 mL
    30 mM 0.0556 mL 0.2779 mL 0.5559 mL 1.3897 mL
    40 mM 0.0417 mL 0.2085 mL 0.4169 mL 1.0423 mL
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    PI3K-IN-1 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.

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    Product Name:
    PI3K-IN-1
    Cat. No.:
    HY-12068
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