Pladienolide B |
Katalog-Nr.GC18780 |
Gezielt bindet Splicing-Faktor 3b und hemmt die mRNA-Spleißung.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 445493-23-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Spliceosomen vermitteln die Verarbeitung von prä-mRNA zu reifer mRNA.[1],[2] Jedes Spliceosom ist ein Mehrkomponenten-Komplex, der mehrere Proteine und RNA-Moleküle enthält, die gemeinsam arbeiten, um Segmente von mRNA wiederholt zu spalten und zusammenzufügen.[1],[3] Pladienolide B ist eine makrocyclische Lactonverbindung, die selektiv an den Splicing-Faktor 3b bindet und die mRNA-Spleißung hemmt.[4],[5] Durch diese Wirkung blockiert Pladienolide B effektiv das Wachstum proliferierender Zellen mit mittleren IC50-Werten von 1,6 nM für sechs Magenkrebszelllinien.[6],[7] In Xenograft-Tumoren, die in Mäusen aus menschlichen Krebszellen erzeugt wurden, blockiert Pladienolide B die mRNA-Spleißung und induziert Apoptose. Die Tumoren werden innerhalb von zwei Wochen nach der Behandlung beseitigt.[7]
References:
[1]. Naro, C., and Sette, C. Phosphorylation-mediated regulation of alternative splicing in cancer. Int.J.Cell Biol. 2013, 1-16 (2013).
[2]. Webb, T.R., Joyner, A.S., and Potter, P.M. The development and application of small molecule modulators of SF3b as therapeutic agents for cancer. Drug Discovery Today 18(1-2), 43-49 (2013).
[4]. Yokoi, A., Kotake, Y., Takahashi, K., et al. Biological validation that SF3b is a target of the antitumor macrolide pladienolide. FEBS Journal 278(24), 4870-4880 (2011).
[5]. Kotake, Y., Sagane, K., Owa, T., et al. Splicing factor SF3b as a target of the antitumor natural product pladienolide. Nature Chemical Biology 3, 570-575 (2007).
[6]. Effenberger, K.A., Anderson, D.D., Bray, W.M., et al. Coherence between cellular responses and in vitro splicing inhibition for the anti-tumor drug pladienolide B and its analogs. The Journal of Biological Chemisty 289, 1938-1947 (2014).
[7]. Sato, M., Muguruma, N., Nakagawa, T., et al. High antitumor activity of pladienolide B and its derivative in gastric cancer. Cancer Science 105(1), 110-116 (2014).
Cas No. | 445493-23-2 | SDF | |
Chemical Name | (4R,7R,8S,9E,11S,12S)-8-(acetyloxy)-4,7-dihydroxy-12-[(1E,3E,5S)-6-[(2R,3R)-3-[(1R,2S)-2-hydroxy-1-methylbutyl]-2-oxiranyl]-1,5-dimethyl-1,3-oxacyclododec-9-en-2-one | ||
Canonical SMILES | O[C@H]1CC(O[C@H](/C(C)=C/C=C/[C@@H](C)C[C@@H]2[C@]([C@H](C)[C@H](CC)O)([H])O2)[C@@H](C)/C=C/[C@H](OC(C)=O)[C@](C)(O)CC1)=O | ||
Formula | C30H48O8 | M.Wt | 536.7 |
Löslichkeit | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 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 | 1.8632 mL | 9.3162 mL | 18.6324 mL |
5 mM | 0.3726 mL | 1.8632 mL | 3.7265 mL |
10 mM | 0.1863 mL | 0.9316 mL | 1.8632 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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 ddH2O, 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.
Average Rating: 5
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