121850 AGL 2263

121850
  
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      Overview

      Replacement Information
      Description
      Overview

      This product has been discontinued.

      We apologize for the inconvenience, but we do not currently have an alternative product. Please refer to our complete listing of receptor tyrosine kinase inhibitors for possible alternatives. Please read the alternative product documentation carefully and contact technical service if you need additional information.





      A cell-permeable benzoxazolone-containing bioisostere of tyrphostin AG 538 (Cat. No. 658403) that acts as a potent, substrate-competitive, but not ATP-competitive, inhibitor of insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R). It is selective towards IR and IGF-1R (IC50 = 0.4 and 0.43 µM, respectively) and inhibits Src and PKB only at much higher concentrations (IC50 = 2.2 and 55 µM, respectively) in kinase assays. Shown to prevent IGF-1-induced cellular IGF-1R autophosphorylation and down stream signalling. Specifically inhibits IGF-1-induced, but not PDGF-induced, activation of PKB in cells. Effectively blocks the formation of colonies in soft agar by breast and prostate cancer cells. Exhibits improved cellular oxidative stability than AG 538.
      Catalogue Number121850
      Brand Family Calbiochem®
      SynonymsAG 2263
      References
      ReferencesBlum, G., et al. 2003. J. Biol. Chem. 278, 40442.
      Product Information
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₇H₁₀N₂O₅
      Chemical formulaC₁₇H₁₀N₂O₅
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary TargetIGF-1R
      Primary Target IC<sub>50</sub>0.43 µM
      Secondary targetIR (IC₅₀ = 0.4 µM) and inhibits Src and PKB at (IC₅₀ = 2.2 and 55 µM, respectively)
      Purity≥97% 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.
      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
      121850

      References

      Reference overview
      Blum, G., et al. 2003. J. Biol. Chem. 278, 40442.
      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.

      Revision08-April-2008 RFH
      SynonymsAG 2263
      DescriptionA cell-permeable, bioisostere of AG 538 (Cat. No. 658403) that acts as a potent, substrate-competitive inhibitor of insulin receptor (IR) tyrosine kinase (IC50 = 400 nM) and insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase (IC50 = 430 nM). Inhibits Src and protein kinase B (PKB/Akt) activities only at higher concentrations (IC50 = 2.2 µM and 55 µM, respectively). Reported to block IGF-1-induced cellular IGF-1R autophosphorylation and downstream signaling. Also reported to specifically inhibit IGF-1-induced, but not PDGF-induced, PKB activation in cells. Shown to effectively block the formation of breast cancer cell and prostate cancer cell colonies in soft agar. Exhibits much improved cellular oxidative stability compared to AG 538.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₀N₂O₅
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (10 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.
      Toxicity Carcinogenic / Teratogenic
      ReferencesBlum, G., et al. 2003. J. Biol. Chem. 278, 40442.