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

Hh Signaling Antagonist XV - CAS 1057677-92-5 - Calbiochem : FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

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

374274
  
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Aperçu

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 SegmentMQ100
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
Référence GTIN
374274 0

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Hh Signaling Antagonist XV - CAS 1057677-92-5 - Calbiochem Certificats d'analyse

TitreNuméro de lot
374274

Références bibliographiques

Aperçu de la référence bibliographique
Miller-Moslin, K., et al. 2009. J. Med. Chem. 52, 3954.
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.

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.