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

Picropodophyllin  (Synonyms: AXL1717; Picropodophyllotoxin; PPP)

Cat. No.: HY-15494 Purity: 99.90%
COA 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
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10 mg USD 119 In-stock
50 mg USD 425 In-stock
100 mg USD 680 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Picropodophyllin:

Top Publications Citing Use of Products

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

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

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

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • 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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    414.41

    Formula

    C22H22O8

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    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:  0.5% CMC-Na/saline water

      Solubility: 3 mg/mL (7.24 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    • 3.

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 2 mg/mL (4.83 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.90%

    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
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    Picropodophyllin 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:
    Picropodophyllin
    Cat. No.:
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