IGF-1R Inhibitor, PPP

$120.00$1,050.00

Product Specification

  • Appearance
    :

    White Solid

  • CAS Number
    :

    477-47-4

  • Cat.number
    :

    VD-OEIA-10002

  • Formula
    :

    C22H22O8

  • MW
    :

    414.4

  • Purity
    :

    ≥95%

  • Solubility
    :

    DMSO or EtOH

  • Storage
    :

    +2°C to +8°C. Protect from light.

  • Synonyms
    :

    Insulin-like Growth Factor-1 Receptor Inhibitor; Picropodophyllin

  • Size
    :

    100mg, 10mg

Product Variations

Product # Price Quantity  
VD-OEIA-10002-0010-10mg $120
VD-OEIA-10002-0100-100mg $1050

Description

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.

1.Mazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432.
2.Vasilcanu, D., et al. 2004. Oncogene 23, 7854.
3.Girnita, A., et al. 2004. Cancer Res. 64, 236.

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