Picropodophyllotoxin

Biological Activity

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

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.

Background References

1. Oncogenic mutations in intestinal adenomas regulate Bim-mediated apoptosis induced by TGF-beta.
   Wiener Z, Band A, Kallio P, Hogstrom J, Hyvonen V, Kaijalainen S, Ritvos O, Haglund C, Kruuna O, Robine S, Louvard D, Ben-Neriah Y, Alitalo K
   Proc Natl Acad Sci U S A, 2014;111(21):E2229-36.
2. Picropodophyllin (PPP) is a potent rhabdomyosarcoma growth inhibitor both in vitro and in vivo
   M Tarnowski, M Tkacz, K Zgutka, J Bujak, P Kopytko, A Pawlik
   BMC Cancer, 2017;17(1):532.
3. IGF-1 degradation by mouse mast cell protease 4 promotes cell death and adverse cardiac remodeling days after a myocardial infarction
   Thor Tejada
   Proc Natl Acad Sci USA, 2016;0(0):.
4. Cyclolignans as inhibitors of the Ins-like growth factor-1 receptor and malignant cell growth.
   Girnita et al.
   Cancer Res., 2004;64:236
5. IGF-1 receptor tyrosine kinase inhibition by the cyclolignan PPP induces G₂/M-phase accumulation and apoptosis in multiple myeloma cells.
   Stromberg et al.
   Blood, 2006;107:669
6. Inhibition of VEGF secretion and experimental choroidal neovascularization by picropodophyllin (PPP), an inhibitor of the Ins-like growth factor-1 receptor.
   Economou et al.
   Invest.Ophthalmol.Vis.Sci., 2008;49:2620

Product Datasheets