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419825 Hh Signaling Antagonist X, Itraconazole - CAS 84625-61-6 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
84625-61-6C₃₅H₃₈Cl₂N₈O₄

Pricing & Availability

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419825-250MG
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      Glass bottle 250 mg
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      Description
      OverviewA cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-α-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~ 0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~ 0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner.
      Catalogue Number419825
      Brand Family Calbiochem®
      Synonyms14LDM Inhibitor, Oriconazole, R51211, Smo Antagonist VII, Sporanox, 14-α-demethylase Inhibitor
      References
      ReferencesKim, J., et al. 2010. Cancer Cell 17, 388.
      Product Information
      CAS number84625-61-6
      FormWhite powder
      Hill FormulaC₃₅H₃₈Cl₂N₈O₄
      Chemical formulaC₃₅H₃₈Cl₂N₈O₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 20/21/22

      Harmful by inhalation, in contact with skin and if swallowed.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Harmful
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstituiton, 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
      Global Trade Item Number
      Catalogue Number GTIN
      419825-250MG 04055977187847

      Documentation

      Hh Signaling Antagonist X, Itraconazole - CAS 84625-61-6 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Hh Signaling Antagonist X, Itraconazole - CAS 84625-61-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      419825

      References

      Reference overview
      Kim, J., et al. 2010. Cancer Cell 17, 388.
      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.

      Revision09-November-2011 RFH
      Synonyms14LDM Inhibitor, Oriconazole, R51211, Smo Antagonist VII, Sporanox, 14-α-demethylase Inhibitor
      DescriptionA cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-α-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number84625-61-6
      Chemical formulaC₃₅H₃₈Cl₂N₈O₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstituiton, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Harmful
      ReferencesKim, J., et al. 2010. Cancer Cell 17, 388.