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506168 p53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem

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CAS #Empirical Formula
91634-12-7C₁₀H₈N₂O

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506168-25MG
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      Description
      OverviewA cell-permeable styrylquinazoline compound that preferentially induces apoptotic death of mutant p53-harboring H1299-His175 and Saos-2-His273 tumor cells (IC50 = 3.4 and 4.9 µM, respectively), while exhibiting much reduced potency towards p53-null (IC50 = 9.6, 11.4, and 14.7 µM against H1299, Saos-2, and HCT116, respectively) or wild-type p53-expressing (IC50 = 13.2 and 20.3 µM against HCT116 and HDF, respectively) cells. STIMA-1 is demonstrated to covalently modify free thiols on mutant p53 in H1299-His175 cells and fully restore its DNA binding activity to the level seen with wild-type p53, resulting in upregulation of p53-dependent gene expression, including p21, PUMA, and Bax.
      Catalogue Number506168
      Brand Family Calbiochem®
      Synonyms2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
      References
      ReferencesZache, N., et al. 2008. Mol. Oncol. 2, 70.
      Product Information
      CAS number91634-12-7
      FormOff-white solid
      Hill FormulaC₁₀H₈N₂O
      Chemical formulaC₁₀H₈N₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 Ambient Temperature Only
      Toxicity Standard Handling
      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 1 week at -20°C. Prepare fresh as required.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      506168-25MG 04055977272345

      Documentation

      p53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      p53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      506168

      Références bibliographiques

      Aperçu de la référence bibliographique
      Zache, N., et al. 2008. Mol. Oncol. 2, 70.
      Fiche technique

      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.

      Revision03-December-2010 RFH
      Synonyms2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
      DescriptionA cell-permeable styrylquinazoline compound that preferentially induces apoptotic death of mutant p53-harboring H1299-His175 and Saos-2-His273 tumor cells (IC50 = 3.4 and 4.9 µM, respectively), while exhibiting much reduced potency towards p53-null (IC50 = 9.6, 11.4, and 14.7 µM against H1299, Saos-2, and HCT116, respectively) or wild-type p53-expressing (IC50 = 13.2 and 20.3 µM against HCT116 and HDF, respectively) cells. STIMA-1 is demonstrated to covalently modify free thiols on mutant p53 in H1299-His175 cells and fully restore its DNA binding activity to the level seen with wild-type p53, resulting in upregulation of p53-dependent gene expression, including p21, PUMA, and Bax.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number91634-12-7
      Chemical formulaC₁₀H₈N₂O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 week at -20°C. Prepare fresh as required.
      Toxicity Standard Handling
      ReferencesZache, N., et al. 2008. Mol. Oncol. 2, 70.