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Indibulin

Cat No. 3728

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Alternative Name: D 24851

Chemical Name: 2-[1-(4-Chlorobenzyl)-1H-indol-3-yl]-2-oxo-N-pyridin-4- ylacetamide

Biological Activity

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

M.Wt:

389.83

Formula:

C₂₂H₁₆CIN₃O₂

Solubility:

Soluble to 25 mM in DMSO

Purity:

>98 %

Storage:

Desiccate at -20°C

CAS No:

[204205-90-3]

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

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

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