[CAS NO. 863774-58-7] Dimethylenastron
PRODUCTS SPECIFICATIONS [863774-58-7]
DESCRIPTION [863774-58-7]
Overview
| MDL | MFCD09264157 |
|---|---|
| Molecular Weight | 302.39 |
| Molecular Formula | C16H18N2O2S |
| SMILES | O=C1C2=C(NC(NC2C3=CC=CC(O)=C3)=S)CC(C)(C)C1 |
1 Publications Citing Use of MCE
Summary
Dimethylenastron is a potent kinesin Eg5 inhibitor, with an IC 50 of 200 nM.
IC50 & Target
|
Eg5 200 nM (IC 50 ) |
In Vitro
Dimethylenastron is a potent Eg5 inhibitor, with an IC 50 of 200 nM. Dimethylenastron exhibits no inhibition of five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped-originating from 4 different organisms). Dimethylenastron (0.5, 1 μM) causes accumulation of cells in G2/M in HeLa cells [1] . Dimethylenastron (3 and 10 μM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dimethylenastron (1.0 µmol) induces a milder scarring but the length of bleb survival is not significantly prolonged compared with the control group. Dimethylenastron (1.0 µmol) reveals a markedly reduced ratio of intraocular pressure and a milder, but not obviously reduced, subconjunctival fibrotic reaction in the rabbits treated with glaucoma filtration surgery [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 330.70 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3070 mL | 16.5349 mL | 33.0699 mL |
| 5 mM | 0.6614 mL | 3.3070 mL | 6.6140 mL |
| 10 mM | 0.3307 mL | 1.6535 mL | 3.3070 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution
References
- [1] Gartner M, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005 Jul;6(7):1173-7.
- [2] Sun XD, et al. Dimethylenastron suppresses human pancreatic cancer cell migration and invasion in vitro via allosteric inhibition of mitotic kinesin Eg5. Acta Pharmacol Sin. 2011 Dec;32(12):1543-8.
- [3] Lüke J, et al. The effect of adjuvant dimethylenastron, a mitotic Kinesin Eg5 inhibitor, in experimental glaucoma filtration surgery. Curr Eye Res. 2010 Dec;35(12):1090-8.