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Dimethylenastron

Cat. No. 5261 1 Citation Submit a Review Datasheet / COA / SDS
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Description: Inhibitor of mitotic motor kinesin Eg5
Chemical Name: 2,3,4,6,7,8-Hexahydro-4-(3-hydroxyphenyl)-7,7-dimethyl-2-thioxo-5(1H)-quinazolinone
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Dimethylenastron

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.

Technical Data for Dimethylenastron

M. Wt 302.39
Formula C16H18N2O2S
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 863774-58-7
PubChem ID 11609157
InChI Key RUOOPLOUUAYNPY-UHFFFAOYSA-N
Smiles O=C1CC(C)(C)CC2=C1C(C3=CC=CC(O)=C3)NC(N2)=S

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.

Solubility Data for Dimethylenastron

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.24 100
ethanol 15.12 50

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 will affect the solvent volumes required to prepare stock solutions.

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

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Product Datasheets for Dimethylenastron

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for Dimethylenastron

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

Kaan et al (2010) Structural basis for inhibition of Eg5 by dihydropyrimidines: stereoselectivity of antimitotic inhibitors enastron, dimethylenastron and fluorastrol. J.Med.Chem. 53 5676 PMID: 20597485

Liu et al (2006) Inhibition of the mitotic kinesin Eg5 up-regulates Hsp70 through the phosphatidylinositol 3-kinase/Akt pathway in multiple myeloma cells. J.Biol.Chem. 281 18090 PMID: 16627469

Sun et al (2011) Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta.Pharmacol Sin. 32 1543 PMID: 21986572

If you know of a relevant reference for Dimethylenastron, please let us know.

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1 Citation for Dimethylenastron

Citations are publications that use Tocris products. Selected citations for Dimethylenastron include:

Simon P et al (2021) Intestinal goblet cells sample and deliver lumenal antigens by regulated endocytic uptake and transcytosis. Elife 10 PMID: 34677124

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Literature in this Area

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