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 10 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.

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

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 NWqzVJdYS3m2b4TvfIlkyqCjc4PhfS=> NVjBfpljUW5idnn0do8h[3m2b4TvfIlkcXS7IHHnZYlve3RidHjlJGEuPTR7IDjoeY1idiCudX7nJINiemOrbn;tZUkhdmWxcHzhd5Rq[yClZXzsJIxqdmVuIFnDOVA:PjBibl2= NEXlWosyPDl6ME[4Ni=>
P-388 neoplastic cell line NX\2NoZpS3m2b4TvfIlkyqCjc4PhfS=> NHPDcJVKdiC4aYTyc{BkgXSxdH;4bYNqfHliYXfhbY5{fCC2aHWgVE0{QDhiKH\yc40hTEKDL{KgcY92e2VrIH7lc5Bt[XO2aXOgZ4VtdCCuaX7lMEBKSzVyPU[wJI5O MUWxOFk5ODZ6Mh?=
HT-29 (human colon carcinoma) neoplastic cell line NIL2XplEgXSxdH;4bYPDqGG|c3H5 M3PwTGlvKH[rdILvJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHSqZTDIWE0zQSBqaIXtZY4h[2:ub36gZ4Fz[2mwb33hLUBv\W:ybHHzeIlkKGOnbHygcIlv\SxiSVO1NF03OCCwTR?= MnT4NVQ6QDB4OEK=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-IGFR1 / p-AKT / p-ERK ; 

PubMed: 22363814     


A) IGFR1 Y1136 Phosphorylation was inhibited with picropodophyllin (PPP). A random pharmacologic control drug, PHA, had no effect on IGFR1 phosphorylation. B) PPP treatment significantly decreases downstream AKT S473 phosphorylation and ERK p44/p42 phosphorylation (C). * denotes P<0.05 compared to control. (n = 3).

22363814
Growth inhibition assay
Cell viability; 

PubMed: 22159423     


Effect of PPP on cell viability. Left panel, cells were treated with 0.5 μM PPP and counted manually in quadruplicates using trypan blue exclusion resulting in number of viable adherent and suspension cells, respectively. Right panel, in parallel, the number of dead adherent and suspension cells was counted and viability calculated and expressed as mean % viable cells ± SD. All experiments were performed three times and one representative is shown.

22159423
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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03646058 Not yet recruiting Drug: Buprenorphine|Drug: Placebo Suicidal Ideation|Major Depressive Episode Centre Hospitalier Universitaire de Nīmes September 2021 Phase 3
NCT04057937 Not yet recruiting Drug: Apremilast|Drug: Placebo Palmoplantaris Pustulosis Celgene September 30 2019 Phase 2
NCT04015518 Recruiting Drug: Spesolimab|Drug: Placebo Palmoplantar Pustulosis (PPP) Boehringer Ingelheim August 14 2019 Phase 2
NCT04061252 Not yet recruiting Drug: KHK4827|Drug: Placebo Palmoplantar Pustulosis Kyowa Kirin Co. Ltd. August 2019 Phase 3
NCT03633396 Recruiting Biological: ANB019|Drug: Placebo Palmoplantar Pustulosis AnaptysBio Inc. May 20 2019 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