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

239825
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      239825-15MG
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          Glass bottle 15 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.
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          239825

          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. 77, 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.

          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 ≤ -70°C
          Protect from light
          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.
          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.