MN58b


Catalog No. size PriceQuantity
M7081-2 2mg solid $152
M7081-10 10mg solid $611

Description

Cas:203192-01-2 (bromide)

roduct Information

MN58b is a selective choline kinase α (CHKα) inhibitor. MN58b is a novel anticancer drug that inhibits choline kinase, resulting in inhibition of phosphocholine synthesis. Inhibition of choline kinase by MN58b resulted in altered phospholipid metabolism both in cultured tumor cells and in vivo.

 

Chemical Formula: C32H40Br2N4

 

Molecular Weight: 640.508

 

Elemental Analysis: C, 60.01; H, 6.30; Br, 24.95; N, 8.75

 

Synonym:

MN58b bromide

MN58b

MN 58b

MN 58b

 

Chemical Name: 1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide

 

InChi Key: 1,1'-((butane-1,4-diylbis(4,1-phenylene))bis(methylene))bis(4-(dimethylamino)pyridin-1-ium) bromide

 

InChi Code: InChI=1S/C32H40N4.2BrH/c1-33(2)31-17-21-35(22-18-31)25-29-13-9-27(10-14-29)7-5-6-8-28-11-15-30(16-12-28)26-36-23-19-32(20-24-36)34(3)4;;/h9-24H,5-8,25-26H2,1-4H3;2*1H/q+2;;/p-2

 

Smiles Code:

CN(C)C1=CC=[N+](C=C1)CC2=CC=C(CCCCC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2.[Br-].[Br-]

 

 

Technical Data:

 

Appearance: 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

Shelf Life: >3 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

The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively.

MN58b (1-5 µM; 72 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) has a marked effect on colony formation at 1 µM, and growth is completely abolished at 5 µM in all the cell lines.

MN58b ((1-10 µM; 24-48 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) induces apoptosis and this response correlates with CHKα expression.

 

In Vivo

MN58b (4 mg/kg; intraperitoneal injection; once a day; for 5 days; MF-1 nude mice) treatment significantly decreases phosphomonoesters in both HT29 and MDA-MB-231 xenografts. Phosphocholine levels are found to correlate with choline kinase activities.

 

 

References

 

  1. Al-Saffar NM, Troy H, Ramírez de Molina A, Jackson LE, Madhu B, Griffiths JR, Leach MO, Workman P, Lacal JC, Judson IR, Chung YL. Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res. 2006 Jan 1;66(1):427-34. doi: 10.1158/0008-5472.CAN-05-1338. PMID: 16397258.

 

  1. Li Y, Kinting S, Höppner S, Forstner ME, Uhl O, Koletzko B, Griese M. Metabolic labelling of choline phospholipids probes ABCA3 transport in lamellar bodies. Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Dec;1864(12):158516. doi: 10.1016/j.bbalip.2019.158516. Epub 2019 Aug 29. PMID: 31473345.

 

  1. Kumar M, Arlauckas SP, Saksena S, Verma G, Ittyerah R, Pickup S, Popov AV, Delikatny EJ, Poptani H. Magnetic resonance spectroscopy for detection of choline kinase inhibition in the treatment of brain tumors. Mol Cancer Ther. 2015 Apr;14(4):899-908. doi: 10.1158/1535-7163.MCT-14-0775. Epub 2015 Feb 5. PMID: 25657334; PMCID: PMC4394035.

 

  1. Guma M, Sanchez-Lopez E, Lodi A, Garcia-Carbonell R, Tiziani S, Karin M, Lacal JC, Firestein GS. Choline kinase inhibition in rheumatoid arthritis. Ann Rheum Dis. 2015 Jul;74(7):1399-407. doi: 10.1136/annrheumdis-2014-205696. Epub 2014 Oct 1. PMID: 25274633; PMCID: PMC4382461.

 

  1. Zimmerman T, Moneriz C, Diez A, Bautista JM, Gómez Del Pulgar T, Cebrián A, Lacal JC. Antiplasmodial activity and mechanism of action of RSM-932A, a promising synergistic inhibitor of Plasmodium falciparum choline kinase. Antimicrob Agents Chemother. 2013 Dec;57(12):5878-88. doi: 10.1128/AAC.00920-13. Epub 2013 Sep 16. PMID: 24041883; PMCID: PMC3837925.

 

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

 

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