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

407247
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      Overview

      Key Spec Table

      Empirical FormulaCAS #
      C₂₂H₂₂O₈477-47-4

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      407247-1MG
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          1 mg
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          Description
          Overview 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.
          Catalogue Number 407247
          Brand Family Calbiochem®
          Synonyms Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
          References
          References 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.
          Product Information
          CAS number 477-47-4
          ATP Competitive N
          Form Off-white solid
          Hill Formula C₂₂H₂₂O₈
          Chemical formula C₂₂H₂₂O₈
          Molar Mass 414.4
          Reversible Y
          Structure formula Image
          Applications
          Biological Information
          Primary Target IGF-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 permeable Y
          Solubility DMSO or EtOH
          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 No
          Special Instructions Following 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

          MSDS

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          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.
          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.

          Revision 09-May-2011 RFH
          Synonyms Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
          Description A 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.
          Form Off-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number 477-47-4
          Molar mass 414.4
          Chemical formula C₂₂H₂₂O₈
          Structure formula
          Purity ≥95% by HPLC
          Solubility DMSO (100 mg/ml) or Ethanol (5 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze No
          Special Instructions Following 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
          References 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.