Picropodophyllin (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

苦鬼臼毒素；AXL1717； Picropodophyllotoxin； PPP

白色粉末

DMSO : 76 mg/mL (183.4 mM)

Ethanol : 1 mg/mL (2.41 mM), warmed

IGF-1R

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. 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. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells.

In SCID mice xenografted with human ES-1, BE, and PC3, Picropodophyllin (20 mg/kg/12 h, i.p.) causes complete tumor regression. In the 5T33MM mouse model, Picropodophyllin also shows a marked antitumor activity, and causes a significant increase in survival.

[1] Girnita A, et al. Cancer Res. 2004, 64(1), 236-242.
[2] Economou, M.A., et al. 2008. Invest. Ophthalmol. Vis. Sci. 49: 2620-2626.
[3] Guha, M., et al. 2007. J. Biol. Chem. 282: 14536-14546.
[4] 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.