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

239820
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₅₄N₈ • 8HCl 155148-31-5

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      239820-5MG
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          5 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          239820

          References

          Reference overview
          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.
          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.

          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 +2°C to +8°C
          Hygroscopic
          Protect from light
          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.