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

Picropodophyllin (Synonyms: AXL1717; Picropodophyllin; PPP)

Cat. No.: HY-15494 Purity: 99.85%
Handling Instructions

Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.

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

Picropodophyllin Chemical Structure

Picropodophyllin Chemical Structure

CAS No. : 477-47-4

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10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 108 In-stock
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50 mg USD 432 In-stock
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100 mg USD 732 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Picropodophyllin purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2016 Feb;37(2):217-27.

    The phosphorylation of IGF-1R is observed by a Western blot assay after the cells are pretreated with PPP 50 nM or a diluent for 60 min and deprived of insulin for 5 min.

    Picropodophyllin purchased from MCE. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176.

    PPP downregulates IGF-1R as well as the total and phosphor-HER2 levels in the MKN7 cell line.
    • Biological Activity

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    • Customer Review

    Description

    Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.

    IC50 & Target

    IC50: 1 nM (IGF-1R)

    In Vitro

    Picropodophyllin (AXL1717) (0.5, 2.5, 10 μM) potently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation in intact cells. Picropodophyllin (AXL1717) also inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells[1]. Picropodophyllin (AXL1717) synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 via further decreasing cell viability and enhancing apoptosis[3]. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells[4].

    In Vivo

    Picropodophyllin (AXL1717) (20 mg/kg/12 h, i.p.) causes complete tumor regression in SCID mice xenografted with human ES-1, BE, and PC3[1]. Picropodophyllin (AXL1717) shows a potent antitumor activity, increases survival in the 5T33MM mouse model[2].

    Molecular Weight

    414.41

    Formula

    C₂₂H₂₂O₈

    CAS No.

    477-47-4

    SMILES

    O=C1OC[[email protected]]2([H])[[email protected]@H](O)C3=C(C=C4OCOC4=C3)[[email protected]@H](C5=CC(OC)=C(OC)C(OC)=C5)[[email protected]@]21[H]

    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 : 50 mg/mL (120.65 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4131 mL 12.0653 mL 24.1307 mL
    5 mM 0.4826 mL 2.4131 mL 4.8261 mL
    10 mM 0.2413 mL 1.2065 mL 2.4131 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [1]

    Four to 5-week-old pathogen-free SCID mice are used and housed within plastic isolators in a sterile facility. ES-1, BE, and PC3 cells (all proved to express IGF-1R), or R-v-src (IGF-1R negative) and P12 (overexpressing IGF-1 and IGF-1R), are injected s.c. at 107 cells/mice in a 0.2 mL volume of sterile saline solution. Immunocompetent Balb-c mice are injected with 107JC murine breast cancer cells per mouse in 0.15 mL volume of sterile saline solution. Experimental treatments with Picropodophyllin (AXL1717) (20 mg/kg/12 h) are performed by daily i.p. injections of the compound in 10 μL volume of DMSO: vegetable oil, 10:1 (v/v). Control mice are treated with the vehicle only. Three animals are treated in each group. Tumor growth is measured every second day using vernier calipers, and the tumor volumes are calculated. The mice are carefully observed for the presence of side effects and are sacrificed at the end of the experiments for histological analysis of the lesions. A separate experiment on Picropodophyllin (AXL1717)-treated (systemically and locally) tumor-free mice, including histological analyses of various organs, confirms previous observations that Picropodophyllin (AXL1717) appears to be nontoxic.

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

    References

    Purity: 99.85%

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    Picropodophyllin
    Cat. No.:
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