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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Dimethylenastron, a quinazoline-thione analog, is a potent, cell-permeable, specific, and reversible mitotic kinesin 5 (Eg5) inhibitor with IC50 of 200 nM. The mitotic motor of ATPase activity stimulated by microtubules is called Eg5. Dimethylenastron, an Eg5 Inhibitor III, has little effect on the ATPase activity of kinesin-1, -4, -7, and -10 and may have anticancer properties. Moreover, dimethylenastron (~1 μM) causes cell cycle arrest and prevents the formation of bipolar spindles in HeLa cells and Xenopus egg extracts. After treatment for 24 hours, dimethylenastron (3 and 10 μM) concentration-dependently suppresses the cancer cells' ability to migrate, but it does not stop the cancer cells from proliferating until 72 hours later. Dimethylenastron also lessens the cancer cells' capacity to invade.
| Targets |
Eg5 (IC50 = 200 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Dimethylenastron has an IC50 of 200 nM, making it a strong Eg5 inhibitor. Five other kinesin subfamilies (kinesin 1/4/7/10 and one ungrouped, originating from four different organisms) are not inhibited by dimethylenastron. In HeLa cells, dimethylenastron (0.5, 1 μM) induces cell accumulation in the G2/M phase.
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| Cell Assay |
Transwell assays measure the invasion of cells in response to dimethylenastron. Matrigel or fibronectin is applied to the transwell filters' upper surface. After adding cells suspended in 200 μL serum-free media to the chamber, the chamber is put in a 24-well plate with the entire medium inside. The matrigel on the upper surface of the filters is removed with cotton swabs once the filters have been gently removed from their 24-hour incubation at 37°C. The cells on the underside of transwell filters are photographed after being fixed for 30 minutes in 4% paraformaldehyde and stained for 10 minutes in 0.1% crystal violet. The number of invading cells is counted in five random fields per filter for quantitative evaluation. The number of invasive cells in the drug-treatment group divided by the number of invasive cells in the control group is used to calculate the extent of cell invasion[2].
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| Animal Protocol |
Following the closure of the conjunctival suture, one of the following agents is injected using a metallic needle (30 G) that is placed into the subconjunctival space at the nasal border of the superior rectus muscle: Following surgery, the rabbits in the control group receive no adjuvant, the other groups receive one unilateral subconjunctival injection of Dimethylenastron (1.0 µmol, 3.0 µmol) or the vehicle (DMSO, 99.9%, 10 mg/mL) alone at baseline. This means that the injection is given immediately after surgery, and in two additional groups, it is given twice more at days 3 and 7 after (1.0 µmol, 3.0 µmol)[3].
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| References |
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| Molecular Formula |
C16H18N2O2S
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| Molecular Weight |
302.39
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| Exact Mass |
302.11
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| Elemental Analysis |
C, 63.55; H, 6.00; N, 9.26; O, 10.58; S, 10.60
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| CAS # |
863774-58-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC1(CC2=C(C(NC(=S)N2)C3=CC(=CC=C3)O)C(=O)C1)C
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| InChi Key |
RUOOPLOUUAYNPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21)
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| Chemical Name |
4-(3-hydroxyphenyl)-7,7-dimethyl-2-sulfanylidene-3,4,6,8-tetrahydro-1H-quinazolin-5-one
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| Synonyms |
Dimethylenastron
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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