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

419825
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
84625-61-6C₃₅H₃₈Cl₂N₈O₄

Products

Catalogue NumberPackaging Qty/Pack
419825-250MG Sklená flaša 250 mg
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 MSDS

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.