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

374274
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      374274-10MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 -20°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 Standard Handling
          ReferencesMiller-Moslin, K., et al. 2009. J. Med. Chem. 52, 3954.