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239820 CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem

CXCR4 Antagonist I, AMD3100, CAS 155148-31-5, is an antagonist of CXCL12 (SDF1) binding to CXCR4 (IC50 = 108 nM for rat CXCR4) and inhibits SDF1-induced Ca2+ flux.

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Synonymes: 1,1ʹ-(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, JM3100

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239820
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Tableau de caractéristiques principal

CAS #Empirical Formula
155148-31-5C₂₈H₅₄N₈ • 8HCl

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      Description
      OverviewA symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC50 = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca2+ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC50 ≤200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC50 = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9. Also available as a 50 mM solution in H2O (Cat. No. 239825).
      Catalogue Number239820
      Brand Family Calbiochem®
      Synonyms1,1ʹ-(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, JM3100
      References
      ReferencesKalatskaya, I., et al. 2009. Mol. Pharmacol. 77, 1240.
      Pitchford, S.C., et al. 2009. Cell Stem Cell 4, 62.
      De Clercq, E. 2009. Biochem. Pharmacol. , 1655.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      De Clercq, E. 2000. Mol. Pharmacol. 57, 833.
      Product Information
      CAS number155148-31-5
      FormOff-white solid
      Hill FormulaC₂₈H₅₄N₈ • 8HCl
      Chemical formulaC₂₈H₅₄N₈ • 8HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationCXCR4 Antagonist I, AMD3100, CAS 155148-31-5, is an antagonist of CXCL12 (SDF1) binding to CXCR4 (IC50 = 108 nM for rat CXCR4) and inhibits SDF1-induced Ca2+ flux.
      Biological Information
      Purity≥98% 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 +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      239820-5MG 04055977198942

      Documentation

      CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      239820

      Références bibliographiques

      Aperçu de la référence bibliographique
      Kalatskaya, I., et al. 2009. Mol. Pharmacol. 77, 1240.
      Pitchford, S.C., et al. 2009. Cell Stem Cell 4, 62.
      De Clercq, E. 2009. Biochem. Pharmacol. , 1655.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      De Clercq, E. 2000. Mol. Pharmacol. 57, 833.
      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.

      Revision10-March-2010 RFH
      Synonyms1,1ʹ-(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, JM3100
      DescriptionA symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC50 = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca2+ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC50 ≤200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC50 = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number155148-31-5
      Chemical formulaC₂₈H₅₄N₈ • 8HCl
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityH₂O (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKalatskaya, I., et al. 2009. Mol. Pharmacol. 77, 1240.
      Pitchford, S.C., et al. 2009. Cell Stem Cell 4, 62.
      De Clercq, E. 2009. Biochem. Pharmacol. , 1655.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      De Clercq, E. 2000. Mol. Pharmacol. 57, 833.