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374274 Hh Signaling Antagonist XV - CAS 1057677-92-5 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(6-(4-(4-Benzylphthalazin-1-yl)piperazin-1-yl)pyridin-3-yl)propan-2-ol, Smo Antagonist VI

374274
  
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      Overview

      Replacement Information
      Description
      Overview

      This product has been discontinued.



      A benzylphthalazinyl compound that blocks the binding of the Smoothened (Smo) agonist Hh-Ag1.5 to Smo in competitive binding assays (IC50 = 5 or 8 nM, respectively, using CHO-K1 membrane expressing murine or human Smo) and potently inhibits Gli-mediated transcription activity upon Hh-Ag1.5 stimulation in TM3-based reporter assays (IC50 = 2.7 or 35 nM, respectively, against 1 or 25 nM Hh-Ag1.5). Shown to exhibit blood-brain barrier permeability and good oral bioavailability in mice and effectively inhibit tumor growth in a dose-dependent manner in a Ptch+/-p53-/- medulloblastoma allograft model in Harlan nu/nu mice (71% regression by two 40 mg/kg oral dosages per day) in vivo.
      Catalogue Number374274
      Brand Family Calbiochem®
      Synonyms2-(6-(4-(4-Benzylphthalazin-1-yl)piperazin-1-yl)pyridin-3-yl)propan-2-ol, Smo Antagonist VI
      References
      ReferencesMiller-Moslin, K., et al. 2009. J. Med. Chem. 52, 3954.
      Product Information
      CAS number1057677-92-5
      FormPale yellow solid
      Hill FormulaC₂₇H₂₉N₅O
      Chemical formulaC₂₇H₂₉N₅O
      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 -20°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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      374274 0

      Documentation

      Hh Signaling Antagonist XV - CAS 1057677-92-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Hh Signaling Antagonist XV - CAS 1057677-92-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      374274

      References

      Reference overview
      Miller-Moslin, K., et al. 2009. J. Med. Chem. 52, 3954.
      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.

      Revision12-April-2011 RFH
      Synonyms2-(6-(4-(4-Benzylphthalazin-1-yl)piperazin-1-yl)pyridin-3-yl)propan-2-ol, Smo Antagonist VI
      DescriptionA benzylphthalazinyl compound that blocks the binding of the Smoothened (Smo) agonist Hh-Ag1.5 to Smo in competitive binding assays (IC50 = 5 or 8 nM, respectively, using CHO-K1 membrane expressing murine or human Smo) and potently inhibits Gli-mediated transcription activity upon Hh-Ag1.5 stimulation in TM3-based reporter assays (IC50 = 2.7 or 35 nM, respectively, against 1 or 25 nM Hh-Ag1.5). Shown to exhibit blood-brain barrier permeability and good oral bioavailability in mice and effectively inhibit tumor growth in a dose-dependent manner in a Ptch+/-p53-/- medulloblastoma allograft model in Harlan nu/nu mice (71% regression by two 40 mg/kg oral dosages per day) in vivo.
      FormPale yellow solid
      CAS number1057677-92-5
      Chemical formulaC₂₇H₂₉N₅O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°C
      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 Standard Handling
      ReferencesMiller-Moslin, K., et al. 2009. J. Med. Chem. 52, 3954.