Picropodophyllotoxin(477-47-4)

Biological activity: Picropodophyllin (PPP, AXL1717) is a selective IGF-1R inhibitor with IC50 of 1nM. It has high selectivity for IGF-IR Chemicalbook, and has no inhibition on IR tyrosine phosphorylation or FGF-R, PDGF-R, EGF-R. Picropodophyllin (PPP) can induce apoptosis and has anti-tumor activity.

In vitro study: In intact cells, PPP effectively inhibits IGF-1R, Akt (Ser473) and Erk1/2 phosphorylation stimulated by IGF-1. In cultured IGF-1R positive tumor cells, Picropodophyllin specifically inhibited cell growth and induced cell apoptosis. Picropodophyllin makes HMCL, primary human MM and mouse 5T33MM cells more sensitive to ABT-737 and ABT-199 by further reducing cell activity and enhancing cell apoptosis. Picropodophyllin and sorafenib synergistically inhibit the proliferation and activity of hepatocellular carcinoma.

In vivo, Picropodophyllin (20mg/kg/12h, i.p.) caused complete tumor degeneration in SCID mice xenotransplanted with human ES-1, BE, and PC3. In the 5T33MM mouse model, Picropodophyllin also showed effective anti-tumor activity and significantly increased the survival rate. White crystalline powder with chemical properties, soluble in methanol, ethanol, DMSO and other organic solvents, and derived from the rhizome of Berberidaceae plant Dysosmaversipellis (Hance.

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