Insulin-like Growth Factor-1 Receptor Inhibitor
Picropodophyllin White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable cis-cyclolignan compound that acts as a non-competitive, potent, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines) and in vivo (complete inhibition of IGF-1R-dependent tumor cell growth at 20 mg/kg/12 hr i.p. in SCID mice) with minimum toxic effect (LD50 > 500 mg/kg). Exhibits little effect towards IR, FGFR, PDGFR and EGFR, and exerts no effects on microtubules and DNA topoisomerase II. Targets the phosphorylation of Y1136 in the activation loop and is the first inhibitor reported to discriminate between IGF-1R and IR. Purity: ≥95% by HPLC. CAS 477-47-4. Ref.: Mazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432. Vasilcanu, D., et al. 2004. Oncogene 23, 7854. Girnita, A., et al. 2004. Cancer Res. 64, 236. |
