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Description: Selective IGF1R inhibitor
Alternative Names: Picropodophyllin
Chemical Name: (5R,5aS,8aR,9R)-5,8,8a,9-Tetrahydro-9-hydroxy-5-(3,4,5-trimethoxyphenyl)-furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
Purity: ≥97% (HPLC)
Citations (3)
Literature (2)
Pathways (1)

Biological Activity for Picropodophyllotoxin

Picropodophyllotoxin is an orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor that exhibits no activity at the insulin receptor, FGFR, PDGFR or EGFR. Inhibits IGF1R autophosphorylation (IC50 ~ 1 nM), increases the fraction of cells in the G2/M phase and upregulates apoptosis. Exhibits antiproliferative effects in multiple cancer cell lines (IC50 = 0.05 - 15 μM), and has anticancer and antineovascularization activity in vivo.

Technical Data for Picropodophyllotoxin

M. Wt 414.41
Formula C22H22O8
Storage Store at +4°C
Purity ≥97% (HPLC)
CAS Number 477-47-4
PubChem ID 72435
Smiles O=C3OC[C@]([C@@]([H])3[C@@H]4[C@]5=CC(OC)=C(OC)C(OC)=C5)([H])[C@@H](O)C1=C4C=C(OCO2)C2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Picropodophyllotoxin

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 41.44 100

Preparing Stock Solutions for Picropodophyllotoxin

The following data is based on the product molecular weight 414.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.41 mL 12.07 mL 24.13 mL
5 mM 0.48 mL 2.41 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets for Picropodophyllotoxin

Certificate of Analysis / Product Datasheet
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References for Picropodophyllotoxin

References are publications that support the biological activity of the product.

Girnita et al (2004) Cyclolignans as inhibitors of the Ins-like growth factor-1 receptor and malignant cell growth. Cancer Res. 64 236 PMID: 14729630

Stromberg et al (2006) IGF-1 receptor tyrosine kinase inhibition by the cyclolignan PPP induces G2/M-phase accumulation and apoptosis in multiple myeloma cells. Blood 107 669 PMID: 16166596

Economou et al (2008) Inhibition of VEGF secretion and experimental choroidal neovascularization by picropodophyllin (PPP), an inhibitor of the Ins-like growth factor-1 receptor. Invest.Ophthalmol.Vis.Sci. 49 2620 PMID: 18515591

If you know of a relevant reference for Picropodophyllotoxin, please let us know.

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View all Insulin and Insulin-like Receptor Inhibitors

Keywords: Picropodophyllotoxin, Picropodophyllotoxin supplier, Selective, IGF1R, inhibitors, inhibits, Receptors, Insulin-like, Receptor, Tyrosine, Kinases, RTKs, Picropodopyhllin, Picropodophyllin, Insulin, and, insulin-like, 2956, Tocris Bioscience

3 Citations for Picropodophyllotoxin

Citations are publications that use Tocris products. Selected citations for Picropodophyllotoxin include:

Stouffer et al (2015) Ins enhances striatal DA release by activating cholinergic interneurons and thereby signals reward. Nat Commun 6 8543 PMID: 26503322

Forster et al (2019) Macrophage-derived Ins.-like growth factor-1 is a key neurotrophic and nerve-sensitizing factor in pain associated with endometriosis. FASEB J fj201900797R PMID: 31291762

Tarnowski (2017) Picropodophyllin (PPP) is a potent rhabdomyosarcoma growth inhibitor both in vitro and in vivo. BMC Cancer 17 532 PMID: 28793874

Do you know of a great paper that uses Picropodophyllotoxin from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Picropodophyllotoxin

Insulin Signaling Pathway

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.