Refametinib R enantiomer |
| رقم الكتالوجGC37516 |
إنانتيومير Refametinib R هو مثبط MEK مستخرج من براءة اختراع WO2007014011A2 ، المركب 1022 ، له EC50 من 2.0-15 نانومتر.
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Cas No.: 923032-38-6
Sample solution is provided at 25 µL, 10mM.
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Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM. MEK|2-15 nM (EC50)
Refametinib R enantiomer is the R enantiomer of Refametinib . Refametinib R enantiomer is an inhibitor of MEK and is useful in treatment of cancer and other hyperproliferative diseases[1].
[1]. Andreas Maderna, et al. N-(arylamino)-sulfonamide inhibitors of mek. WO 2007014011 A2.
Kinase experiment: | A typical 25 μL assay contains 0.002 nmol MEK1, 0.02 nmol ERK2, 0.25 nmol MBP, 0.25 nmol unlabeled ATP, and 0.1 μCi [γ33P] ATP. The screening assay essentially comprised four additions. Five μL of diluted compound are dispensed to 96-well assay plates. Ten μL of 2.5× enzyme cocktail (MEKl and ERK2 only) are then added to each well followed by a pre- incubation for 30 minutes at ambient temperature. Ten μL of 2.5× substrate cocktail (labeled and unlabeled ATP plus MBP) are then added, followed by incubation for 60 minutes at ambient temperature. Finally, 100 μL of 10% trichloroacetic acid (TCA) are added and incubated for 30 minutes at room temperature to halt the reaction and precipitate radiolabeled protein products. Reaction products are harvested on glass fiber 96 well filter plates prewetted with water and 1% pyrophosphate. The filter plate is then washed 5 times with water. Water is displaced by absolute ethanol and the plate is allowed to air dry for 30 minutes at room temperature. A back seal is applied manually and 40 μL of scintillation cocktail are dispensed to each well. A top seal is applied and the plate is counted in the TopCount for two seconds per well. For certain experiments a truncated version of MEK that requires activation by Raf kinase are used[1]. |
Cell experiment: | Effects of compounds in the cell are determined by Western blotting for phosphorylated ERK. MDA-MB-231 breast cancer cells are plated in a 48 well plate at 20,000 cells per well and grown in a 37° humidified CO2 incubator. The following day, the growth media (DMEM+10% fetal bovine serum) is removed and replaced with starve media (DMEM+0.1% fetal bovine serum). Cells are incubated in the starve media for sixteen hours and then treated with a range of compound concentrations for thirty minutes. After incubation with compound, cells are stimulated with 100ng/mL EGF for five minutes. The cells are then lysed and analyzed by Western blot using a monoclonal antibody raised to phosphorylated ERK. The signal is amplified using a secondary antibody conjugated to a near-IR dye and detected on a Licor Odyssey scanner. The intensity of signal is quantitated and this data is used to generate dose response curves and EC50 calculations[1]. |
References: [1]. Andreas Maderna, et al. N-(arylamino)-sulfonamide inhibitors of mek. WO 2007014011 A2. | |
| Cas No. | 923032-38-6 | SDF | |
| Canonical SMILES | O=S(C1(C[C@H](CO)O)CC1)(NC(C(NC(C(F)=C2)=CC=C2I)=C3F)=C(OC)C=C3F)=O | ||
| Formula | C19H20F3IN2O5S | M.Wt | 572.34 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7472 mL | 8.7361 mL | 17.4721 mL |
| 5 mM | 0.3494 mL | 1.7472 mL | 3.4944 mL |
| 10 mM | 0.1747 mL | 0.8736 mL | 1.7472 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
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