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239825 InSolution™ CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem

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239825-15MG
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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.
      Catalogue Number239825
      Brand Family Calbiochem®
      Synonyms1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 8HCl, 4H₂O, 1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O
      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. 77, 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
      FormLiquid
      FormulationA 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.
      Hill FormulaC₂₈H₅₄N₈ • 8HCl • 4H₂O
      Chemical formulaC₂₈H₅₄N₈ • 8HCl • 4H₂O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCXCR4
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Dry Ice Only
      Toxicity Standard Handling
      Storage ≤ -70°C
      Protect from Light Protect from light
      Avoid freeze/thaw Avoid freeze/thaw
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      239825-15MG 04055977198997

      Documentation

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

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

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

      TitreNuméro de lot
      239825

      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. 77, 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.

      Revision19-March-2013 JSW
      Synonyms1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 8HCl, 4H₂O, 1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O
      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.
      FormLiquid
      FormulationA 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number155148-31-5
      Chemical formulaC₂₈H₅₄N₈ • 8HCl • 4H₂O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      Storage Protect from light
      Avoid freeze/thaw
      ≤ -70°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°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. 77, 1655.
      Thoma, G., et al. 2008. J. Med. Chem. 51, 7915.
      De Clercq, E. 2000. Mol. Pharmacol. 57, 833.