A potent and selective inhibitor of insulin-like growth factor 1 receptor (IGF-1R, IC50=6 nM). It efficiently blocks IGF-1R activity, reduces pAKT and pERK1/2, induces apoptosis in IGF-1R-positive tumor cells and causes complete tumor regression in xenografted and allografted mice. Picropodophyllin downregulates IGF-1R by interfering with the action of β-arrestin 1/MDM2. It causes tumor regression and attenuates invasiveness of uveal melanoma cells. It displays beneficial effects on tumor growth, angiogenesis, bone disease and survival in a mouse multiple myeloma model. It attenuates intimal hyperplasia after vascular injury. Inhibition of IGF-1R is non-competitive with ATP.
Product Details
| Formula: | C22H22O8 |
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| MW: | 414.4 |
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| CAS: | 477-47-4 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | White solid |
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| Solubility: | Soluble in DMSO (10mg/ml, warm) or dimethyl formamide (25mg/ml) |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Picropodophyllin induces downregulation of the insulin-like growth factor 1 receptor: potential mechanistic involvement of Mdm2 and beta-arrestin1: R. Vasilcanu, et al.; Oncogene
27, 1629 (2008),
Abstract;
Targeting the IGF-1R using picropodophyllin in the therapeutical 5T2MM mouse model of multiple myeloma: beneficial effects on tumor growth, angiogenesis, bone disease and survival: E. Menu, et al.; Int. J. Cancer
121, 1857 (2007),
Abstract;
The cyclolignan picropodophyllin attenuates intimal hyperplasia after rat carotid balloon injury by blocking insulin-like growth factor-1 receptor signaling: A. Razuvaev, et al.; J. Vasc. Surg.
46, 108 (2007),
Abstract;
The insulin-like growth factor-I receptor inhibitor picropodophyllin causes tumor regression and attenuates mechanisms involved in invasion of uveal melanoma cells: A. Girnita, et al.; Clin. Cancer Res.
12, 2 (2006),
Abstract;
Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth: A. Girnita, et al.; Cancer Res.
64, 236 (2004),
Abstract;
