Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
Other Sizes |
|
Targets |
SUV39H2/KMT1B
|
---|---|
ln Vitro |
At an IC50 of 0.67 μM, OTS186935 hydrochloride inhibits the proliferation of A549 cells[1].
|
ln Vivo |
In xenograft models created from human cancer cell lines, OTS186935 hydrochloride (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) shows growth inhibition [1].
|
Animal Protocol |
Animal/Disease Models: Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )[1]
Doses: 10 mg/kg Route of Administration: intravenously (iv); one time/day for 14 days Experimental Results: Tumor growth inhibition of 42.6% on day 14 . Animal/Disease Models: Female BALB/cAJcl-nu/nu (nude) mice (bearing A549 cells)[1] Doses: 25 mg/kg Route of Administration: intravenously (iv); one time/day for 14 days Experimental Results: Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity. |
References |
[1]. Vougiouklakis T, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831.
|
Molecular Formula |
C25H26CLN5O2.8/5HCL
|
---|---|
Molecular Weight |
522.31
|
Related CAS # |
OTS186935;2093400-18-9;OTS186935 trihydrochloride;2093401-85-3
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
H2O :~50 mg/mL (~95.73 mM)
DMSO :~25 mg/mL (~47.86 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (3.98 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (191.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9146 mL | 9.5729 mL | 19.1457 mL | |
5 mM | 0.3829 mL | 1.9146 mL | 3.8291 mL | |
10 mM | 0.1915 mL | 0.9573 mL | 1.9146 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.