Indibulin

Biological Activity

Indibulin is a microtubule destabilizer that blocks tubulin polymerization (IC₅₀ = 0.3 μM). Blocks cell cycle progression at metaphase and displays antitumor activity against a variety of malignancies in vitro (IC₅₀ values ranging from 0.036 - 0.285 μM). Induces complete tumor remission in the Yoshida AH13 rat sarcoma model in vivo. Lacks neurotoxicity due to an ability to discriminate between posttranslationally modified tubulin in mature neuronal microtubules and less-modified tubulin present in immature neuronal or nonneuronal microtubules. Displays oral availability and efficacy towards MDR tumor cells.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. D-24851, a novel synthetic microtubule inhibitor, exerts curative antitumoral activity in vivo, shows efficacy toward multidrug-resistant tumor cells, and lacks neurotoxicity.
   Bacher et al.
   Cancer Res., 2001;61:392
2. Microtubule inhibitor D-24851 induces p53-independent apoptotic cell death in malignant glioma cells through Bcl-2 phosphorylation and Bax translocation.
   Kanzawa et al.
   Int.J.Oncol., 2005;26:589
3. Indibulin, a novel microtubule inhibitor, discriminates between mature and nonneuronal tubulin.
   Wienecke and Bacher
   Cancer Res., 2009;69:171

Product Datasheets