407247 IGF-1R Inhibitor, PPP - CAS 477-47-4 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₂H₂₂O₈ 477-47-4

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407247-1MG
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      Description
      OverviewA 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.
      Catalogue Number407247
      Brand Family Calbiochem®
      SynonymsInsulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
      References
      ReferencesMazitschek, 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.
      Product Information
      CAS number477-47-4
      ATP CompetitiveN
      FormOff-white solid
      Hill FormulaC₂₂H₂₂O₈
      Chemical formulaC₂₂H₂₂O₈
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationIGF-1R Inhibitor, PPP, CAS 477-47-4, is a cell-permeable, substrate competitive, reversible, potent, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay) & in vivo.
      Biological Information
      Primary TargetIGF-1R both in vitro and in vivo
      Primary Target IC<sub>50</sub>1 nM against IGF-1R in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Carcinogenic / Teratogenic
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in solution at room temperature.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      IGF-1R Inhibitor, PPP - CAS 477-47-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      IGF-1R Inhibitor, PPP - CAS 477-47-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      407247

      References

      Reference overview
      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.

      Brochure

      Title
      Insulin Pathway Poster PDF ( 618 KB )
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-May-2011 RFH
      SynonymsInsulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
      DescriptionA cell-permeable, reversible, potent, substrate competitive, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay; ≤60 nM and 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 only minimal toxic effects (LD50 >500 mg/kg). Exhibits little inhibition 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number477-47-4
      Chemical formulaC₂₂H₂₂O₈
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in solution at room temperature.
      Toxicity Carcinogenic / Teratogenic
      ReferencesMazitschek, 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.