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Tubulysin D

Katalog-Nr.GC37838

Tubulysin D ist eines der potentesten Derivate unter den Tubulysinen, die aus den myxobakteriellen Arten Arrangium geophyra und Angiococcus disciformis isoliert wurden. Tubulysin D ist ein neuartiges Tetrapeptid, das eine starke AntitumoraktivitÄt aufweist und durch Hemmung der Tubulinpolymerisation mit einem IC50 von 1,7 μM zu Zellzyklusstillstand und Apoptose fÜhrt. Tubulysin zeigt eine Äußerst starke zytotoxische AktivitÄt in SÄugerzellen, einschließlich multiresistenter Zelllinien, mit IC50-Werten im unteren nanomolaren Bereich.

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Tubulysin D Chemische Struktur

Cas No.: 309935-57-7

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. IC50: 1.7 μM (Tubulin)[1]

Tubulysin D has IC50s of 4.7 pM, 3.1 pM, 670 pM and 13 pM for HL60, HCT116, MCF7, A549 cell lines antiproliferative activity, respectively[1].

[1]. Shibue T, et al. Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline. Bioorg Med Chem Lett. 2011 Jan 1;21(1):431-4. [2]. Kubicek K, et al. The tubulin-bound structure of the antimitotic drug tubulysin. Angew Chem Int Ed Engl. 2010 Jun 28;49(28):4809-12.

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