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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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

239820
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Overview

Replacement Information

Key Spec Table

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

Products

Catalogue NumberPackaging Qty/Pack
239820-5MG 5 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. 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
Catalogue Number GTIN
239820-5MG 04055977198942

Documentation

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

Title

Safety Data Sheet (SDS) 

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