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Refametinib R enantiomer

MEK1/2 allosteric inhibitor CAS# 923032-38-6

Refametinib R enantiomer

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Chemical structure

Refametinib R enantiomer

3D structure

Chemical Properties of Refametinib R enantiomer

Cas No. 923032-38-6 SDF Download SDF
PubChem ID 15985330 Appearance Powder
Formula C19H20F3IN2O5S M.Wt 572.34
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BAY 869766 R enantiomer; RDEA119 R enantiomer
Solubility Soluble in DMSO
Chemical Name N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
SMILES COC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)CC(CO)O)NC3=C(C=C(C=C3)I)F)F)F
Standard InChIKey RDSACQWTXKSHJT-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H20F3IN2O5S/c1-30-15-7-13(21)16(22)18(24-14-3-2-10(23)6-12(14)20)17(15)25-31(28,29)19(4-5-19)8-11(27)9-26/h2-3,6-7,11,24-27H,4-5,8-9H2,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Refametinib R enantiomer

DescriptionRefametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.In Vitro: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].

References:
[1]. Andreas Maderna, et al. N-(arylamino)-sulfonamide inhibitors of mek. WO 2007014011 A2.

Protocol

Kinase Assay [1]
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 Assay [1]
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.

Refametinib R enantiomer Dilution Calculator

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Refametinib R enantiomer Molarity Calculator

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Preparing Stock Solutions of Refametinib R enantiomer

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7472 mL 8.7361 mL 17.4721 mL 34.9443 mL 43.6803 mL
5 mM 0.3494 mL 1.7472 mL 3.4944 mL 6.9889 mL 8.7361 mL
10 mM 0.1747 mL 0.8736 mL 1.7472 mL 3.4944 mL 4.368 mL
50 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.6989 mL 0.8736 mL
100 mM 0.0175 mL 0.0874 mL 0.1747 mL 0.3494 mL 0.4368 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Refametinib R enantiomer

Refametinib R enantiomer (RDEA119/BAY 869766) is a potent, selective and allosteric inhibitor of MEK1/2 in enzyme inhibition assays with IC50 values of 19 nmol/L and 47 nmol/L for MEK1 and MEK2, respectively [1].

Refametinib R enantiomer has been reported to inhibit MEK activity with EC50 values of 8.7±0.7nmol/L, 5.1±1.1nmol/L, 8.7±1nmol/L, 2.5±1.7nmol/L, 3.8±1.7nmol/L and 15.8±2.4nmol/L for A375, A431, SK-Mel-28, Colo205, HT-29 and BxPC3 cells, respectively. Furthermore, Refametinib R enantiomer has been revealed to inhibit anchorage-dependent growth with GI50 values ranging from 67 to 89nmol/L in human cancer cell lines (A375, A431, Colo205, and HT-29 cells). Moreover, Refametinib R enantiomer has shown a potent tumor growth inhibition (TGI) in the human A375 and colon carcinoma Colo205 tumor xenograft models [1].

References:
[1] Iverson C1, Larson G, Lai C, Yeh LT, Dadson C, Weingarten P, Appleby T, Vo T, Maderna A, Vernier JM, Hamatake R, Miner JN, Quart B. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 2009 Sep 1;69(17):6839-47.

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Description

Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM.

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