121762 AG 957, Adamantyl Ester

121762
  
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      Overview

      Replacement Information
      Description
      Overview

      This product has been discontinued.

      Please refer to our complete listing of Protein Tyrosine Kinase Inhibitors for a possible alternative. Please read the alternative product documentation carefully and contact technical service if you need additional information.





      A lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 121761) that displays antiproliferative properties. Shown to be selective and ~3-4 fold more potent than the bcr/abl kinase inhibitor AG 957. Has a longer serum half-life in vivo. Downregulates p210bcr/abl autokinase activity (IC50 = 14 µM). Selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. Reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC50 ~0.1-0.25 µM).
      Catalogue Number121762
      Brand Family Calbiochem®
      Synonyms4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate, 4-(2,5-Dihydroxy-benzylamino)benzoic Acid Adamantan-1-yl Ester
      References
      ReferencesAvramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
      Mow, B.M., et al. 2002. Blood 99, 664.
      Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.
      Product Information
      FormOff-white solid
      Hill FormulaC₂₄H₂₇NO₄
      Chemical formulaC₂₄H₂₇NO₄
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary Targetp210bcr-abl
      Primary Target IC<sub>50</sub>14 µM
      Secondary targetSelectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC₅₀ = 9.8 µM)
      Purity≥ 97% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Blue Ice Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 weeks at -20°C. Ethanol 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
      121762

      References

      Reference overview
      Avramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
      Mow, B.M., et al. 2002. Blood 99, 664.
      Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.
      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.

      Revision02-June-2010 JSW
      Synonyms4-Amino-N-(2,5-dihydroxybenzyl)adamantyl Benzoate, 4-(2,5-Dihydroxy-benzylamino)benzoic Acid Adamantan-1-yl Ester
      DescriptionA lipophilic, adamantyl ester form of tyrphostin AG 957 (Cat. No. 121761) that displays anti-proliferative properties. Shown to be selective and ~3-4 fold more potent than AG 957 as a bcr/abl kinase inhibitor. Also exhibits a longer serum half-life in vivo. Down-regulates p210bcr/abl autokinase activity (IC50 = 14 µM), selectively blocks granulocyte colony formation in chronic myelogenous leukemia (CML) progenitors (median IC50 = 12 µM), and inhibits proliferation of K562 cells (IC50 = 9.8 µM) by inducing apoptosis. Also blocks protein synthesis and VEGF secretion. Reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC50 ~100-250 nM).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₄H₂₇NO₄
      Structure formulaStructure formula
      Purity≥ 97% by HPLC
      SolubilityDMSO (10 mg/ml) or Ethanol (5 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 3 weeks at -20°C. Ethanol stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAvramis, I.A., et al. 2002. Cancer Chemother. Pharmacol. 50, 479.
      Mow, B.M., et al. 2002. Blood 99, 664.
      Svingen, P.A., et al. 2000. Clin. Cancer Res. 6, 237.