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Pladienolide B

Katalog-Nr.GC18780

Gezielt bindet Splicing-Faktor 3b und hemmt die mRNA-Spleißung.

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Pladienolide B Chemische Struktur

Cas No.: 445493-23-2

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500μg
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100μg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

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.

Complete Stock Solution Preparation Table

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
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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. )

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