Home Immunology & Inflammation CXCR antagonist MSX-122 For research use only.

MSX-122

Synonyms: Q-122

MSX-122 (Q-122) is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

MSX-122 Chemical Structure

MSX-122 Chemical Structure

CAS No. 897657-95-3

Purity & Quality Control

MSX-122 Related Products

Signaling Pathway

CXCR Signaling Pathways

CXCR Signaling Pathway

Biological Activity

Description MSX-122 (Q-122) is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
Targets
CXCR4 [1]
~10 nM
In vitro
In vitro

MSX-122 is also incapable of blocking the binding of 125I-labeled CXCL12 to CXCR4. MSX-122 appears to be insufficiently large to block all binding sites between CXCR4 and CXCL12. MSX-122 blocks certain CXCR4 functions via binding to the CXCL12-binding site and interfering with CXCR4/CXCL12-mediated signaling. MSX-122 can intervene in the Gαi-signaling pathway (cAMP modulation), but not the Gq-pathway (calcium flux)[1].
Cell Research Cell lines MDA-MB-231 cells
Concentrations 1, 10, 100, and 1000 nM
Incubation Time 15 mins
Method

For binding affinity assay, MDA-MB-231 cells cultured in an 8-well slide chamber are preincubated with MSX-122 at 1, 10, 100, and 1000 nM. Then the cells are fixed with 4% formaldehyde and incubated with 50 nM biotinylated TN14003, and followed by Rhodamine staining.
In Vivo
In vivo

MSX-122 blocks bleomycin-induced lung fibrosis involving chemotaxis and homing of CXCR4-positive mesenchymal progenitor cells into the lungs. MSX-122 exhibits anti-inflammatory activity in a carrageenan-induced paw edema model. MSX-122 blocks lung metastasis of breast cancer and SCCHN, and liver metastasis of uveal melanoma in vivo[1].
Animal Research Animal Models Male C57BL/6 mice (age 5–6 weeks)
Dosages 10 mg/kg
Administration i.p. injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00591682 Suspended
Solid Tumors
Metastatix Inc.
 November 2007 Phase 1

Chemical Information & Solubility

Molecular Weight 292.34 Formula

C16H16N6
CAS No. 897657-95-3 SDF --
Smiles C1=CN=C(N=C1)NCC2=CC=C(C=C2)CNC3=NC=CC=N3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 3 mg/mL ( (10.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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