MP-A08 (Synonyms: NSC 122314) |
رقم الكتالوجGC33016
One-Click Copy Product Info
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MP-A08 هو مثبط انتقائي للغاية من مثبطات سفينجوزين كيناز (SPHK1) الذي يستهدف كلاً من SphK1 و SphK2 بقيم Ki تبلغ 6.9 ± 0.8 ميكرومتر و 27 ± 3 ميكرومتر ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 219832-49-2
Sample solution is provided at 25 µL, 10mM.
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MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SphK1 and SphK2 with Kivalues of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.In vitro:MP-A08 blocks pro-proliferative signalling pathways, induces mitochondrial-associated apoptosis in a SK-dependent manner, and reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis. MP-A08 inhibit SphK2, cause a decrease in EC barrier integrity in vitro in both cell type.[2]In vivo: MP-A08 suppresses the growth of human lung tumor xenografts in mice.
[1]. Pitman MR et al. A selective ATP-competitive sphingosine kinase inhibitor demonstrates anti-cancer properties. Oncotarget, 2015 Mar 30, 6(9):7065-83. [2]. Dimasi DP et al. Examining the Role of Sphingosine Kinase-2 in the Regulation of Endothelial Cell Barrier Integrity. Microcirculation, 2016 Apr, 23(3):248-65.
| Cas No. | 219832-49-2 | SDF | |
| المرادفات | NSC 122314 | ||
| Canonical SMILES | O=S(C1=CC=C(C)C=C1)(NC2=CC=CC=C2/C=N/C3=CC=CC=C3NS(=O)(C4=CC=C(C)C=C4)=O)=O | ||
| Formula | C27H25N3O4S2 | M.Wt | 519.64 |
| الذوبان | DMSO : ≥ 50 mg/mL (96.22 mM);Water : < 0.1 mg/mL (insoluble) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9244 mL | 9.622 mL | 19.2441 mL |
| 5 mM | 384.9 μL | 1.9244 mL | 3.8488 mL |
| 10 mM | 192.4 μL | 962.2 μL | 1.9244 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)