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PicropodophyllotoxinCat. No. 2956 |
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Alternative Name: Picropodopyhllin 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 |
Biological Activity
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.Certificate of Analysis / Safety Data Sheet
References
Girnita et al (2004) Cyclolignans as inhibitors of the insulin-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 insulin-like growth factor-1 receptor. Invest.Ophthalmol.Vis.Sci. 49 2620. PMID: 18515591.
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Keywords: Picropodophyllotoxin, supplier, Selective, IGF1R, inhibitors, Receptors, Insulin-like, Receptor, Tyrosine, Kinases, RTKs
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