MSX-122


Catalog No. size PriceQuantity
M6597-2 2mg solid $103
M6597-10 10mg solid $391

Description

Cas:897657-95-3

Product Information

MSX-122 is a n orally bioavailable inhibitor of CXCR4 with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the GPCR (G protein-coupled receptor) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; it is also a co-receptor for HIV entry into T cells. The chemical structure of MSX-122 is very similar to that of WZ811.

 

Chemical Formula: C16H16N6

 

Exact Mass: 292.14364

 

Molecular Weight: 292.34 

 

Elemental Analysis: C, 65.74; H, 5.52; N, 28.75

 

Synonym: 

 

MSX122

MSX 122

MSX-122

 

Chemical Name:

N,N'-(1,4-phenylenebis(methylene))bis(pyrimidin-2-amine)

 

InChi Key:

PXZXYRKDDXKDTK-UHFFFAOYSA-N

 

InChi Code:  InChI=1S/C16H16N6/c1-7-17-15(18-8-1)21-11-13-3-5-14(6-4-13)12-22-16-19-9-2-10-20-16/h1-10H,11-12H2,(H,17,18,21)(H,19,20,22)

 

Smiles Code:

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

 

 

Technical Data:

 

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life:>2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

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.

 

 

References

 

  1. Shu HK, Yoon Y, Hong S, Xu K, Gao H, Hao C, Torres-Gonzalez E, Nayra C, Rojas M, Shim H. Inhibition of the CXCL12/CXCR4-Axis as Preventive Therapy for Radiation-Induced Pulmonary Fibrosis. PLoS One. 2013 Nov 7;8(11):e79768. doi: 10.1371/journal.pone.0079768. PubMed PMID: 24244561; PubMed Central PMCID: PMC3820649.

 

  1. Ziarek JJ, Liu Y, Smith E, Zhang G, Peterson FC, Chen J, Yu Y, Chen Y, Volkman BF, Li R. Fragment-based optimization of small molecule CXCL12 inhibitors for antagonizing the CXCL12/CXCR4 interaction. Curr Top Med Chem. 2012;12(24):2727-40. PubMed PMID: 23368099; PubMed Central PMCID: PMC3839847.

 

  1. Liang Z, Zhan W, Zhu A, Yoon Y, Lin S, Sasaki M, Klapproth JM, Yang H, Grossniklaus HE, Xu J, Rojas M, Voll RJ, Goodman MM, Arrendale RF, Liu J, Yun CC, Snyder JP, Liotta DC, Shim H. Development of a unique small molecule modulator of CXCR4. PLoS One. 2012;7(4):e34038. doi: 10.1371/journal.pone.0034038. Epub 2012 Apr 2. PubMed PMID: 22485156; PubMed Central PMCID: PMC3317778.

 

Products are for research use only. Not for human use.

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