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Insulin receptor inhibitor
BML-EI372-0001 1 mg 223.00 USD
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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

Purity:≥98% (HPLC)
Appearance:White solid
Solubility:Soluble in DMSO (10mg/ml, warm) or dimethyl formamide (25mg/ml)
Shipping:Ambient Temperature
Long Term Storage:-20°C
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;