2. MAPK/ERK Pathway
  3. MEK
  4. Refametinib

Refametinib  (Synonyms: BAY 869766; RDEA119)

製品番号: HY-14691 純度: 99.82%
COA 取扱説明書 Technical Support

Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.

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CAS 番号 : 923032-37-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 在庫あり
Solution
10 mM * 1 mL in DMSO USD 94 在庫あり
Solid
5 mg $75 在庫あり
10 mg $110 在庫あり
25 mg $190 在庫あり
50 mg $300 在庫あり
100 mg $440 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of Refametinib:

Refametinib 関連抗体

Top Publications Citing Use of Products

    Refametinib purchased from MedChemExpress. Usage Cited in: Appl Sci. 2023 Mar 29, 13(7), 4340.

    Refametinib (50 nM; 1 h) significantly decreases cell viability in SCC4 Cells.

    Refametinib purchased from MedChemExpress. Usage Cited in: Appl Sci. 2023 Mar 29, 13(7), 4340.

    Refametinib (50 nM; 1 h) significantly increases the expression of PARP and Caspase-3 in SCC4 Cells.

    MEK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.

    IC50 & Target[1]

    MEK1

    19 nM (IC50)

    MEK2

    47 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A549 CC50
    > 100 μM
    Compound: 54; RDEA-119
    Cytotoxicity against human A549 cells
    Cytotoxicity against human A549 cells
    		[PMID: 33539089]
    体外実験

    Refametinib (BAY 869766; RDEA119) selectively binds directly to an allosteric pocket in the MEK1/2 enzymes. Refametinib potently inhibits MEK activity in enzyme inhibition assays in a non-ATP-competitive manner (MEK1 IC50=19 nM, MEK2 IC50=47 nM) determined through incorporation of radioactive phosphate from ATP into ERK as substrate. Refametinib potently inhibits MEK activity as measured by phosphorylation of ERK1/2 across several human cancer cell lines of different tissue origins and BRAF mutational status with EC50 values ranging from 2.5 to 15.8 nM. Refametinib inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 values ranging from 67 to 89 nM. In contrast, Refametinib has significantly less growth-inhibitory potency against cell lines with wild-type BRAF (A431 cells) or MDA-MB-231 cells harboring a BRAF mutation G464V that shows minimal (<2-fold increase) enhancement of inherent kinase activity. Under anchorage-independent conditions, GI50 values for all cell lines tested are similar (40-84 nM). MDA-MB-231 and A431 cells are significantly more sensitive to Refametinib under anchorage-independent conditions[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Refametinib 関連抗体
    体内実験

    Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, highly selective inhibitor of MEK1/2, which is active in human tumor xenograft models and is well tolerated within the therapeutic exposure range in animals[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    572.34

    分子式

    C19H20F3IN2O5S
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    O=S(C1(C[C@H](O)CO)CC1)(NC(C(NC(C(F)=C2)=CC=C2I)=C3F)=C(OC)C=C3F)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 31 mg/mL (54.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.82%

    COA (253 KB) HNMR (189 KB) LCMS (177 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    MEK1 kinase activity is determined using mERK2 K52A T183A as the substrate. Recombinant MEK1 enzyme (5 nM) is first activated by 0.02 unit or 1.5 nM of RAF1 in the presence of 25 mM HEPES (pH 7.8), 1 mM MgCl2, 50 mM NaCl, 0.2 mM EDTA, and 50 μM ATP for 30 min at 25°C. The reactions are initiated by adding 2 μM of mERK2 K52A T183A and 2.5 μCi [γ-33P]ATP in a total volume of 20 μL. The MEK2 kinase activity is determined similarly except that activation by RAF1 is not needed and 11 nM of MEK2 enzyme (active) are used in the assays. Kinase profiling is performed. The Z'-LYTE biochemical assay is used. Refametinib is assayed in quadruplicate at 10 μM against 205 kinases[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    For anchorage-dependent growth inhibition experiments, A375, SK-Mel-28, A431, Colo205, HT-29, MDA-MB-231, and BxPC3 cell lines are plated in white 384-well plates at 1,000/20 μL/well or white 96-well microplates at 4,000/100 μL/well. After 24-h incubation at 37°C, 5% CO2, and 100% humidity, Refametinib is incubated for 48 h at 37°C and assayed using CellTiter-Glo. For the 96-well anchorage-independent growth assay, wells of an “ultralow binding” plate are filled with 60 μL of a 0.15% agarose solution in complete RPMI 1640. Then, 60 μL of complete RPMI 1640 containing 9,000 cells in 0.15% agarose are added per well. After 24 h, 60 μL of a 3× drug solution in agarose-free complete RPMI 1640 are added. After 7 d, 36 μL of 6× MTS reagent are added per well. After 2 h at 37°C, absorbance at 490 nm is determined on the M5 plate reader. Nonlinear curve fitting is performed using GraphPad Prism 4[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice[1]
    Female athymic nude mice are used for all the efficacy studies except for the Colo205 study 2, which used male mice. Mice are injected s.c. in the flank with 1×106 tumor cells (Colo205 and A431) or ~1 mm3 tumor fragments (A375 and HT-29). Tumor volumes are monitored by caliper measurements. For efficacy analysis, treatment is initiated when tumors are 80 to 185 mm3. Refametinib (25 and 50 mg/kg/d) is administered by oral gavage once daily or twice daily for 14 d or once every 2 d for 14 doses[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7472 mL 8.7361 mL 17.4721 mL 43.6803 mL
    5 mM 0.3494 mL 1.7472 mL 3.4944 mL 8.7361 mL
    10 mM 0.1747 mL 0.8736 mL 1.7472 mL 4.3680 mL
    15 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9120 mL
    20 mM 0.0874 mL 0.4368 mL 0.8736 mL 2.1840 mL
    25 mM 0.0699 mL 0.3494 mL 0.6989 mL 1.7472 mL
    30 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4560 mL
    40 mM 0.0437 mL 0.2184 mL 0.4368 mL 1.0920 mL
    50 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8736 mL
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    Refametinib Related Classifications

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Refametinib923032-37-5BAY 869766 RDEA119BAY869766BAY-869766RDEA119RDEA 119RDEA-119MEKMitogen-activated protein kinase kinaseMAPKKMAP2KallostericMEK1MEK2orallynon-ATP-competitivetumorInhibitorinhibitorinhibit

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    製品番号:
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