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Novel inhibitor of tubulin polymerization; cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). Prevents growth of tumor models in mice following oral administration in vivo.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 251.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.98 mL||19.9 mL||39.8 mL|
|5 mM||0.8 mL||3.98 mL||7.96 mL|
|10 mM||0.4 mL||1.99 mL||3.98 mL|
|50 mM||0.08 mL||0.4 mL||0.8 mL|
References are publications that support the biological activity of the product.
Beckers et al (2002) 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. Cancer Res. 62 3113 PMID: 12036922
Mahboobi et al (2001) Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. J.Med.Chem. 44 4535 PMID: 11741473
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Keywords: D-64131, D-64131 supplier, inhibitors, inhibits, tubulin, polymerization, Antitumor, Tau, Microtubules, Mitosis, 1643, Tocris Bioscience
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The antitumoral efficacy of D-64131 in comparison to paclitaxel and vincristine was evaluated in resistance mediated by the MRP and in human tumor cells with resistance to cisplatin, the topoisomerase I inhibitor SN-38 (7-ethyl-10-hydroxycamptothecin) and the thymidylate synthase inhibitors 5-fluorouracil and raltitexed.
Literature in this Area
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