1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

MSX-122 

Cat. No.: HY-13696 Purity: 99.74%
Handling Instructions

MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.

For research use only. We do not sell to patients.

MSX-122 Chemical Structure

MSX-122 Chemical Structure

CAS No. : 897657-95-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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  • Protocol

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  • References

Description

MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.

IC50 & Target[1]

CXCR4/CXCL12

∼10 nM (IC50)

In Vitro

MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 shows no inhibition on cAMP reduction mediated by their corresponding ligands CCR3/CCL5 and CCR5/CCL5. MSX-122 (100 nM) potently blocks invasion of 78% MDA-MB-231 cells. However, MSX-122 does not suppress T-tropic HIV infection and is inactive in calcium flux assay[1].

In Vivo

MSX-122 (10 mg/kg, i.p.) blocks inflammation induced by carrageenan and lung fibrosis induced by bleomycin in mice. MSX-122 (4 mg/kg, i.p., daily) blocks metastasis in an experimental animal model of breast cancer metastasis. Furthermore, MSX-122 (10 mg/kg i.p., daily) significantly decreases the numbers of hepatic micrometastases[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4207 mL 17.1034 mL 34.2067 mL
5 mM 0.6841 mL 3.4207 mL 6.8413 mL
10 mM 0.3421 mL 1.7103 mL 3.4207 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
Six- to eight-week-old female nude mice are given injections of 1.5×106 MDA-MB-231 breast cancer cells mixed with the compound (1 µM, less than 5 min preincubation) through the tail vein (10/group). From the following day, mice in the treated group are given 4 mg/kg MSX-122ms (salt form) daily by i.p. injection. The animals are sacrificed 35 days after the tumor cell injection. Whole lung tissues are harvested and sectioned for real-time RT-PCR for human CXCR4 and H&E histostaining to evaluate the metastatic tumor area in five fields per section microscopically. These experiments are repeated once more to confirm the results. For the head and neck cancer animal model, metastatic subclones of 686LN-Ms cells are injected in the same way as MDA-MB-231 cells. [18F]FDG-PET is performed. For the uveal melanoma micrometastasis mouse model, on day 0, each mouse is inoculated with 1×106 wild-type OMM2.3 cells expressing HGF/TGF-β/CXCR4/MMP2 into the posterior chamber of right eye. On day 3, mice are treated with 10 mg/kg MSX-122 in 0.1 mL volume of 45% CD daily by i.p. injection, whereas the control mice are injected with 0.1 mL 45% CD only. On day 7, eyes with tumor are enucleated. The growth of tumor is checked by histological methods. On day 28, hepatic tissues are collected and fixed in 10% formalin, processed, H&E stained, and the number of hepatic micrometastases is counted under microscope. Six sections through the center of the liver are microscopically examined for the presence of micrometastases (<100 µm diameter) and the average number of micrometastases per section is determined. Ten mice per group are used. A table summarizing animal experiments for three metastasis models can be found in the Data S3[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

292.34

Formula

C₁₆H₁₆N₆

CAS No.

897657-95-3

SMILES

C1(CNC2=NC=CC=N2)=CC=C(CNC3=NC=CC=N3)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
MSX-122
Cat. No.:
HY-13696
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MSX-122

Cat. No.: HY-13696