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

Overview

Replacement Information

Products

Catalog NumberPackaging Qty/Pack
239825-15MG Glass bottle 15 mg
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®
Synonyms1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O, 1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 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
Catalog Number GTIN
239825-15MG 04055977198997

Documentation

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

Title

Safety Data Sheet (SDS) 

InSolution™ CXCR4 Antagonist I, AMD3100 - CAS 155148-31-5 - Calbiochem 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
Synonyms1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O, 1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 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.