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MSX-122 CXCR antagonist

Cat.No.S6617

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

Chemical Structure

Molecular Weight: 292.34

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 292.34 Formula

C16H16N6

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 897657-95-3 -- Storage of Stock Solutions

Synonyms Q-122 Smiles C1=CN=C(N=C1)NCC2=CC=C(C=C2)CNC3=NC=CC=N3

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (10.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
CXCR4 [1]
~10 nM
In vitro

MSX-122 is also incapable of blocking the binding of 125I-labeled CXCL12 to CXCR4. This compound appears to be insufficiently large to block all binding sites between CXCR4 and CXCL12. It blocks certain CXCR4 functions via binding to the CXCL12-binding site and interfering with CXCR4/CXCL12-mediated signaling. This chemical can intervene in the Gαi-signaling pathway (cAMP modulation), but not the Gq-pathway (calcium flux)[1].

In vivo

MSX-122 blocks bleomycin-induced lung fibrosis involving chemotaxis and homing of CXCR4-positive mesenchymal progenitor cells into the lungs. This compound exhibits anti-inflammatory activity in a carrageenan-induced paw edema model. It blocks lung metastasis of breast cancer and SCCHN, and liver metastasis of uveal melanoma in vivo[1].

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00591682 Suspended
Solid Tumors
Metastatix Inc.
November 2007 Phase 1

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