Refametinib R enantiomerMEK1/2 allosteric inhibitor CAS# 923032-38-6 |
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Quality Control & MSDS
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Chemical structure
![Refametinib R enantiomer](/media/images/struct/BCC4055.png)
3D structure
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. |
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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. |
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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. |
Description | Refametinib 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: |
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Refametinib R enantiomer Dilution Calculator
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Refametinib R enantiomer Molarity Calculator
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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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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