| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Refametinib R enantiomer targets MEK1 and MEK2, key kinases in the MAPK/ERK signaling pathway. It is a potent, non-ATP-competitive, allosteric inhibitor with IC50 values of 19 nM for MEK1 and 47 nM for MEK2, and an EC50 of 2.0-15 nM. By inhibiting MEK, it disrupts the signaling cascade and inhibits the growth of cancer cells.
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|---|---|
| ln Vitro |
The R-enantiomer of refametinib is known as Refametinib R-enantiomer. A MEK inhibitor called refametinib R enantiomer is used to treat hyperproliferative disorders such cancer [1].
In vitro, Refametinib R enantiomer demonstrates potent inhibition of MEK1/2 activity. It has an EC50 of 2.0-15 nM. It inhibits anchorage-dependent growth and has shown activity against human A375 melanoma and Colo205 colon carcinoma cell lines. |
| ln Vivo |
In vivo, Refametinib R enantiomer has shown efficacy in human A375 melanoma and Colo205 colon carcinoma tumor xenograft models. It is an inhibitor of MEK and is useful in the treatment of cancer and other hyperproliferative diseases.
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| Enzyme Assay |
The in vitro MEK kinase assay involves incubating the enzyme with a substrate (e.g., ERK) and ATP in the presence of varying concentrations of Refametinib R enantiomer. The amount of phosphorylated substrate is measured, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for Refametinib R enantiomer utilize cancer cell lines such as A375 melanoma and Colo205 colon carcinoma. Cells are treated with the compound, and cell viability is assessed by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal experiments for Refametinib R enantiomer are performed in xenograft models using human A375 melanoma or Colo205 colon carcinoma cells. The compound is administered orally, and tumor growth is monitored.
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| ADME/Pharmacokinetics |
Refametinib R enantiomer has a molecular weight of 572.34 g/mol and is soluble in DMSO. It is typically stored as a powder at -20°C. Its purity is >98%.
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| Toxicity/Toxicokinetics |
Toxicological data for Refametinib R enantiomer are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
Refametinib R enantiomer is a research compound with no clinical approval. It is a valuable tool for studying MEK1/2 biology and the role of the MAPK/ERK signaling pathway in cancer. It is used in drug discovery programs to explore the therapeutic potential of MEK inhibitors for the treatment of cancer and other hyperproliferative diseases.
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| Molecular Formula |
C₁₉H₂₀F₃IN₂O₅S
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|---|---|
| Molecular Weight |
572.34
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| Exact Mass |
572.008
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| CAS # |
923032-38-6
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| Related CAS # |
Refametinib;923032-37-5
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| PubChem CID |
50912933
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
566.9±60.0 °C at 760 mmHg
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| Flash Point |
296.7±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
4.78
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
31
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| Complexity |
711
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C1(CC1)C[C@@H](O)CO)(=O)(=O)NC1=C(OC)C=C(F)C(F)=C1NC1C=CC(I)=CC=1F
|
| InChi Key |
RDSACQWTXKSHJT-LLVKDONJSA-N
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| InChi Code |
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/t11-/m1/s1
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| Chemical Name |
N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2R)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide
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| Synonyms |
BAY 869766 R enantiomerRDEA 119 BAY 869766 R enantiomer BAY-69766R enantiomerBAY869766 BAY 86 9766 BAY 86-9766BAY869766RDEA-119
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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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