Picropodophyllin (PPP)

Catalog No.S7668 Synonyms: AXL1717

Picropodophyllin (PPP) Chemical Structure

Molecular Weight(MW): 414.41

Picropodophyllin (PPP) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R).

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Cited by 7 Publications

4 Customer Reviews

  • CLL B cells purified from freshly isolated or freeze-thawed PBMCs from CLL patient samples were treated with a single dose of 1 µM PPP and were immunoblotted for the expression of phosphorylated IGF1R and IRS-1 (n = 4).

    Blood, 2013, 122(9):1621-33. Picropodophyllin (PPP) purchased from Selleck.

    (E): Expression levels of NANOG and p-IGF-IR were measured by immunoblotting in HCT116 and SW620 cells after treatment with IGF-II or PPP.

    Stem Cells, 2016, 34(4):820-31.. Picropodophyllin (PPP) purchased from Selleck.

  • In an MTT assay, a combined treatment co‐targeting HER2 and IGF‐1R produced a synergistic effect in MKN7 cells. In this assay, the concentrations of afatinib, neratinib, and picropodophyllin (PPP) were all 500 nmol/L, and the cells were exposed to the drugs for 3 days. MKN7 cells, cultured under the same conditions as in the MTT assay, were stained using crystal violet (photographs).

    Cancer Sci, 2018, 109(4):1166-1176. Picropodophyllin (PPP) purchased from Selleck.

    Representative blots for phosphorylation of IGF1R Tyr980 and PKB Ser473 in primary hepatocytes from liver-specific AMPKa1/a2 knockout and AMPKa1f/f/a2f/f mice in the presence or absence of PPP.

    FEBS J, 2017, 284(13):2096-2109. Picropodophyllin (PPP) purchased from Selleck.

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Biological Activity

Description Picropodophyllin (PPP) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R).
Targets
IGF-1R [1]
(Cell-free assay)
1 nM
In vitro

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A-549 (human lung carcinoma) neoplastic cell line MofFR5l1d3SxeHnjxsBie3OjeR?= NXPnW|g6UW5idnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RidHjlJGEuPTR7IDjoeY1idiCudX7nJINiemOrbn;tZUkhdmWxcHzhd5Rq[yClZXzsJIxqdmVuIFnDOVA:PjBibl2= NXy4OmZnOTR7OEC2PFI>
P-388 neoplastic cell line NEj5O5JEgXSxdH;4bYPDqGG|c3H5 M{Tv[mlvKH[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHSqZTDQMVM5QCBqZoLvcUBFSkFxMjDtc5V{\SlibnXvdIxie3SrYzDj[YxtKGyrbnWsJGlEPTB;NkCgcm0> M3\MblE1QThyNkiy
HT-29 (human colon carcinoma) neoplastic cell line NY[xSXV1S3m2b4TvfIlkyqCjc4PhfS=> NHuwdnJKdiC4aYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCC2aHWgTHQuOjliKHj1cYFvKGOxbH;uJINiemOrbn;tZUkhdmWxcHzhd5Rq[yClZXzsJIxqdmVuIFnDOVA:PjBibl2= Ml3ENVQ6QDB4OEK=

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:

[1]

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In vitro tyrosine kinase assays.:

Assay of IGF-1R-catalyzed substrate phosphorylation of pTG, using a 96-well plate tyrosine kinase assay kit, is performed. We use recombinant epidermal growth factor receptor, immunoprecipitated IR from HEPG2, immunoprecipitated IGF-1R from P6 cells, and IGF-1R immunodepleted supernatant from P6 (representing “non-IGF-1R tyrosine kinases”). After 30-min treatment of the receptors with the desired compounds in the kinase buffer [50 mM HEPES buffer (pH 7.4), 20 mM MgCl2, 0.1 MnCl2, and 0.2 Na3VO4], the kinase reaction is activated by addition of ATP. The phosphorylated polymer substrate is probed with a phosphotyrosine-specific monoclonal antibody conjugated to horseradish peroxidase, clone PT-66. Color is developed with horseradish peroxidase chromogenic substrate O-phenylenediamine dihydrochloride and quantitated by spectrophotometry (ELISA reader). IGF-1R tyrosine autophosphorylation is analyzed by a sandwich ELISA assay. Briefly, 96-well plates are coated overnight at 4°C with 1 μg/well of an antibody to IGF-1R β-subunit. The plates are blocked with 1% BSA in PBS Tween for 1 h, and then 80 μg/well of total protein lysate from the P6 cell line is added. As a negative control we use total protein lysate from the R- cell line. The investigated compounds are added in tyrosine kinase buffer without ATP at room temperature for 30 min before kinase activation with ATP. Kinase assay is performed using the Sigma kit (see above). After spectrophotometry the IC50 values of inhibitors are determined using the REGRESSION function of Statistica program.
Cell Research:

[1]

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  • Cell lines: Melanoma cells (FM 55, SK-MEL-28, SK-MEL-5, C8161, DFB, DFW and AA), sarcoma cells (RD-ES), breast carcinoma cells (MCF 7), prostate carcinoma cells (PC3), hepatoma cells (HepG2) and embryonic mouse fibroblasts (P6 and R-)
  • Concentrations: ~15 μM
  • Incubation Time: 48 hours
  • Method:

    The determinations are performed using the Cell proliferation kit II, which is based on colorimetric change of the yellow tetrazolium salt 2,3-bis[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide inner salt in orange formazan dye by the respiratory chain of viable cell. All of the standards and experiments are performed in triplicates.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: SCID mice bearing ES-1, BE, or PC3 xenografts that express IGF-1R, or R- v-src (IGF-1R negative) and P12 (overexpressing IGF-1 and IGF-1R)
  • Formulation: DMSO:vegetable oil, 10:1 (v/v)
  • Dosages: 20 mg/kg/12 h
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL warmed (197.87 mM)
Ethanol 1 mg/mL warmed (2.41 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 414.41
Formula

C22H22O8

CAS No. 477-47-4
Storage powder
in solvent
Synonyms AXL1717

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03618979 Recruiting Low Back Pain Regenexx LLC January 2019 Not Applicable
NCT03763851 Not yet recruiting Metastatic Prostate Cancer|Lung Cancer|Breast Cancer Tetra Bio-Pharma|Santé Cannabis|McGill University January 1 2019 Not Applicable
NCT03618979 Recruiting Low Back Pain Regenexx LLC January 2019 Not Applicable
NCT03763851 Not yet recruiting Metastatic Prostate Cancer|Lung Cancer|Breast Cancer Tetra Bio-Pharma|Santé Cannabis|McGill University January 1 2019 Not Applicable
NCT03564548 Not yet recruiting Cancer|Breakthrough Cancer Pain Tetra Bio-Pharma|Santé Cannabis December 1 2018 Phase 2
NCT03564548 Not yet recruiting Cancer|Breakthrough Cancer Pain Tetra Bio-Pharma|Santé Cannabis December 1 2018 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I am currently setting the conditions for in vivo experiments, how should I reconstitute the drug?

  • Answer:

    Other than DMSO:vegetable oil 10:1 (v/v) cited from reference. We tested another formulation: 4% DMSO+corn oil. S7668 Picropodophyllin (PPP) can be dissolved in it at 5 mg/ml clearly. But after stayed for about 20-30 min, the two phase would separate and wouldn't get together again. So if you are going to use this formulation, please prepare the fresh solution just before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID