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Picropodophyllin (PPP)
Catalog No.S7668 Synonyms: AXL1717
For research use only.
Picropodophyllin (PPP, AXL1717) 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). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity.
CAS No. 477-47-4
Selleck's Picropodophyllin (PPP) has been cited by 32 publications
Purity & Quality Control
Choose Selective IGF-1R Inhibitors
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Biological Activity
| Description | Picropodophyllin (PPP, AXL1717) 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). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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 (from reference)
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 414.41 | ||
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| Formula | C22H22O8 |
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| CAS No. | 477-47-4 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | COC1=CC(=CC(=C1OC)OC)C2C3C(COC3=O)C(C4=CC5=C(C=C24)OCO5)O | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05174065 | Not yet recruiting | Drug: Apremilast|Drug: Placebo | Palmoplantar Pustulosis | Amgen | February 17 2022 | Phase 3 |
| NCT04433052 | Not yet recruiting | Behavioral: personalised prevention program (PPP) | Coronary Heart Disease | Tampere University | October 2021 | Not Applicable |
| NCT03646058 | Recruiting | Drug: Buprenorphine|Drug: Placebo | Suicidal Ideation|Major Depressive Episode | Centre Hospitalier Universitaire de Nīmes | September 2021 | Phase 3 |
| NCT04842084 | Recruiting | Biological: Blood samples | Healthy Volunteers | Centre Hospitalier Universitaire de Saint Etienne | April 23 2021 | -- |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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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