MN58b |
カタログ番号GC38406
One-Click Copy Product Info
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MN58bは選択的コリンキナーゼα（CHKα）阻害剤であり、ホスホコリン合成を阻害します。 MN58b は、アポトーシスの誘導により細胞増殖を抑制し、抗腫瘍活性も持っています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 203192-01-2
Sample solution is provided at 25 µL, 10mM.
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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].
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
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]
[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.
| Cas No. | 203192-01-2 | SDF | |
| Canonical SMILES | 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-] | ||
| Formula | C32H40Br2N4 | M.Wt | 640.49 |
| 溶解度 | DMSO: 14.71 mg/mL (22.97 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5613 mL | 7.8065 mL | 15.613 mL |
| 5 mM | 312.3 μL | 1.5613 mL | 3.1226 mL |
| 10 mM | 156.1 μL | 780.7 μL | 1.5613 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)