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MN58b

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Chemical Structure| 203192-01-2 同义名 : -
CAS号 : 203192-01-2
货号 : A1251823
分子式 : C32H40Br2N4
纯度 : 98%
分子量 : 640.495
MDL号 : MFCD32215299
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(23.42 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Choline kinase plays a key role in the regulation of membrane phospholipid synthesis and has oncogenic properties in vitro. The expression level of CHKα is increased in a large number of human humors [3]. MN58b is a CHKα inhibitor that inhibits phosphocholine synthesis and reduced cell growth through induction of apoptosis. The sensitivity of cells to MN58b is correlated to the expression of CHKα protein. In a panel of 12 PDAC cell lines, the IC50s of MN58b ranged from 0.23 to 3.2μM. The IC50s of MN58b for parental and resistant cells was 3.14 μM and 0.77 μM, respectively[4]. In the experiment with MDA-MB-231 cells, after 48-hour treatment with 6μM MN58b, the percentage of cells in G1 phase was statistically significantly increased, whereas the percentage of cells in S and G2 phases was decreased[5]. In murine models, the increased levels of CHKα significantly reduced survival of mice with bladder cancer, while after the treatment with MN58b at dose of 5mg/kg, i.p.. A significant inhibition of tumor growth was observed, as well as relevant increased in survival[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.56mL

0.31mL

0.16mL

7.81mL

1.56mL

0.78mL

15.61mL

3.12mL

1.56mL
参考文献

[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.

[3]Lacal J. C., et al. Choline Kinase α Inhibitors MN58b and RSM932A enhances the Antitumor Response to Cisplatin in Lung Tumor Cells. Pharmaceutics. 2022, 14(6), 1143.

[4]Mazarico, J. M., et al. Choline Kinase Alpha (CHKα) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors. Mol Cancer Ther. 2006. 15(2), 323-333.

[5]AI-Saffar, N. M. S., et al. Noninvasive Magnetic Resonance Spectroscopic Pharmacodynamic Markers of the Choline Kinase Inhibitor MN58b in Human Carcinoma Models. Cancer Res. 2006. 66(1), 427-434.

[6]Hernando, E., et al. A critical role for choline kinase-α in the aggressiveness of bladder carcinomas. Oncogene. 2009. 28, 2425-2435.