Picropodophyllotoxin
IGF1R inhibitor / Potent and selective inhibitor of insulin-like growth factor 1 receptor (IGF1R) which is non-competitive with ATP1. Displays no activity at IR, EGFR, FGFR or PDGFR. Inhibits IGF1R autophosphorylation IC50 ~ 1 nM1. Displays antiproliferative activity in numerous tumor cell lines, IC50 = 0.05 - 15 uM2. Exhibits antiangiogenic activitiy3. Attenuates intimal hyperplasia after vascular injury4. Active in vivo.
Biochemicals & reagents
477-47-4
1) Girnita et al. (2004), Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth; Cancer Res., 64 236 2) Girnita et al. (2006), The insulin-like growth factor-I receptor inhibitor picropodophyllin causes tumor regression and attenuates mechanisms involved in invasion of iveal melanoma cells; Clin. Cancer Res., 12 1383 3) Menu et al. (2007), Targeting the IGF-1R using picropodophyllin in therapeutical 5T2MM mouse model of multiple myeloma: beneficial effects on tumor growth, angiogenesis, bone disease and survival; Int. J. Cancer, 121 1857 4) Razuvaev et al. (2007), The cyclolignan picropodophyllin attenuates intimal hyperplasia after rat carotid balloon injury by blocking insulin-like growth factor-1 receptor signaling; J. Vasc. Surg., 46 108
RT
TARGET: Kinase; Cytoskeleton -- PATHWAY: Cell cycle; Proliferation -- RESEARCH AREA: Angiogenesis -- DISEASE AREA: Cancer