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

PQ401 

Cat. No.: HY-13686 Purity: 99.88%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 127 In-stock
Estimated Time of Arrival: December 31
10 mg USD 115 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PQ401 purchased from MCE. Usage Cited in: Nature Cancer. 2020 Jan.

    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

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    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.

    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].

    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.

    196868-63-0

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 14.29 mg/mL (41.81 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2926 mL 1.4629 mL 2.9258 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: ≥ 1.43 mg/mL (4.18 mM); Clear solution

    • 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

    • 3.

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

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

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

    PQ401PQ 401PQ-401IGF-1RApoptosisInsulin-like growth factor-1 receptorautophosphorylationMCF-7cellsbreastcancercaspaseapoptosisInhibitorinhibitorinhibit

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