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407247  IGF-1R Inhibitor, PPP

Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin

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17 April 2014

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Product number Qty/Pk
407247-1MG  1 mg 
A cell-permeable cis-cyclolignan compound that acts as a substrate competitive, reversible, 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.
Product information
Form Off-white solid
Primary Target IGF-1R both in vitro
Primary Target IC50 1 nM in cell-free kinase assay
Molar mass 414.4
Protect from Light Yes
Packaged under inert gas Yes
Cell permeable Yes
Purity ≥95% by HPLC
Solubility DMSO or EtOH
Chemical formula C22H22O8
CAS number 477-47-4
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Carcinogenic / Teratogenic
IGF-1R Inhibitor, PPP, molecular structure

© Merck KGaA, Darmstadt, Germany, 2014


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