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

407247
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₂₂H₂₂O₈477-47-4

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      407247-1MG
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          Glass bottle 1 mg
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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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          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 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.