Dimethylenastron

Product Description

Dimethylenastron is an inhibitor of mitotic motor kinesin Eg5 (IC₅₀ = 200 nM). Arrests mitosis, triggers apoptosis and up-regulates Hsp-70 expression in multiple human myeloma cell lines. Also inhibits the growth of several types of cancer cell lines (EC₅₀ values are 330, 603, 743 and 881 nM in HCT116, Htert-HME1, BxPC3, K562 and NCI-H1299 cancer cells, respectively). Suppresses the migration and invasion of PANC1 cells in vitro. Cytoprotective.

Solubility

Preparing Stock Solutions for Dimethylenastron

The following data is based on the product molecular weight 302.39

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.31 mL	16.53 mL	33.07 mL
5 mM	0.66 mL	3.31 mL	6.61 mL
10 mM	0.33 mL	1.65 mL	3.31 mL
50 mM	0.07 mL	0.33 mL	0.66 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Liu Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells. J.Biol.Chem. 2006 PMID: 16627469
• Sun Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta.Pharmacol Sin. 2011 PMID: 21986572
• Kaan Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J.Med.Chem. 2010 PMID: 20597485