MN58b

Modify Date: 2024-01-06 17:29:20

MN58b Structure
MN58b structure
Common Name MN58b
CAS Number 203192-01-2 Molecular Weight 640.49
Density N/A Boiling Point N/A
Molecular Formula C32H40Br2N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MN58b


MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].

 Names

Name MN58b

 MN58b Biological Activity

Description MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].
Related Catalog
Target

Choline kinase α (CHKα)[1]

In Vitro The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively[1]. 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[1]. 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[1]. Cell Viability Assay[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 5 µM Incubation Time: 72 hours Result: Inhibited cells growth. Apoptosis Analysis[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells Concentration: 1 µM, 2 µM, 5 µM, 10 µM Incubation Time: 24 and 48 hours Result: Induced cell apoptosis.
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[2]. Animal Model: MF-1 nude mice with HT29 or MDA-MB-231 cells[2] Dosage: 4 mg/kg Administration: Intraperitoneal injection; once a day; for 5 days Result: Phosphomonoesters decreased significantly.
References

[1]. Mazarico JM, et al. Choline Kinase Alpha (CHKα) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors. Mol Cancer Ther. 2016 Feb;15(2):323-33.

[2]. Al-Saffar NM, et al. 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.

 Chemical & Physical Properties

Molecular Formula C32H40Br2N4
Molecular Weight 640.49

 Safety Information

Hazard Codes Xi