2. Protein Tyrosine Kinase/RTK Apoptosis
  3. IGF-1R Apoptosis
  4. PQ401

PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.

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

PQ401 Chemical Structure

PQ401 Chemical Structure

CAS No. : 196868-63-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 70 In-stock
10 mg USD 115 In-stock
50 mg USD 350 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

PQ401 Related Antibodies

Top Publications Citing Use of Products

    PQ401 purchased from MedChemExpress. Usage Cited in: Nature Cancer. 75-85 (2020).

    LLC cells cultured under normal or STS-like conditions in the presence of 1 µg/mL rIGF-1, PQ401 (500 ng/mL), their combination or vehicle. GAPDH was used as a control. This experiment was performed once.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis[1].

    IC50 & Target

    IGF-IR; apoptosis[1]
    In Vitro

    PQ401 (1, 5, 10, 25, and 50 μM; 3 days) inhibits proliferation of cultured MCF-7 cells grown in serum or IGF-I in MCF-7 cells[1].
    Twenty-four hours of treatment with 15 μM PQ401 induces caspase-mediated apoptosis[1].
    PQ401 inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1 μM.

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

    PQ401 Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: Breast cancer cells, MCF-7 cells
    Concentration: 1, 5, 10, 25, and 50 μM
    Incubation Time: 3 days
    Result: Significantly reduced proliferation (IC50, 8 μM) at concentrations in the range of 1 μM.
    Produced a dramatic reduction in cell number from pretreatment levels at concentrations >10 μM.
    In Vivo

    PQ401 (50 or 100 mg/kg; i.p.; thrice a week) results in a significant dose-dependent reduction in tumor growth over the course of the study. PQ401 reduces the growth rate of MCNeuA cells implanted into mice[1].

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

    Animal Model: Female mice were MCNeuA tumor cells[1]
    Dosage: 50 or 100 mg/kg
    Administration: Administered i.p. thrice a week; 24 days
    Result: Resulted in a significant dose-dependent reduction in tumor growth. Tumor growth in the animals treated with 100 mg/kg was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals.
    Molecular Weight

    341.79

    Formula

    C18H16ClN3O2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=C(OC)C=CC(Cl)=C3
    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 : 14.29 mg/mL (41.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (2.93 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9258 mL 14.6289 mL 29.2577 mL
    5 mM 0.5852 mL 2.9258 mL 5.8515 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.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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: ≥ 1.43 mg/mL (4.18 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: 1.43 mg/mL (4.18 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.43 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 (14.3 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 8.33 mg/mL (24.37 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (14.63 mM); Suspended solution; Need ultrasonic

    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: 99.85%

    COA (261 KB) LCMS (265 KB)

    Handling Instructions (2659 KB)
    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
    H2O / DMSO 1 mM 2.9258 mL 14.6289 mL 29.2577 mL 73.1443 mL
    DMSO 5 mM 0.5852 mL 2.9258 mL 5.8515 mL 14.6289 mL
    10 mM 0.2926 mL 1.4629 mL 2.9258 mL 7.3144 mL
    15 mM 0.1951 mL 0.9753 mL 1.9505 mL 4.8763 mL
    20 mM 0.1463 mL 0.7314 mL 1.4629 mL 3.6572 mL
    25 mM 0.1170 mL 0.5852 mL 1.1703 mL 2.9258 mL
    30 mM 0.0975 mL 0.4876 mL 0.9753 mL 2.4381 mL
    40 mM 0.0731 mL 0.3657 mL 0.7314 mL 1.8286 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    PQ401 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:

    PQ401196868-63-0PQ 401PQ-401IGF-1RApoptosisInsulin-like growth factor-1 receptorautophosphorylationMCF-7cellsbreastcancercaspaseapoptosisInhibitorinhibitorinhibit

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