2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Remibrutinib

Remibrutinib  (Synonyms: LOU064)

製品番号: HY-128757 純度: 99.76%
COA 取扱説明書 Technical Support

Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.

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CAS 番号 : 1787294-07-8

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 391 在庫あり
Solution
10 mM * 1 mL in DMSO USD 391 在庫あり
Solid
1 mg $166 在庫あり
5 mg $350 在庫あり
10 mg $550 在庫あり
50 mg $980 在庫あり
100 mg $1480 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Remibrutinib 関連抗体

Top Publications Citing Use of Products

    Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421.

    Concentration response of phosphorylated (pBTK) inhibition by PTBTK3 (n = 3) and remibrutinib (n = 3) in JeKo-1 cells.

    Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421.

    Uptake of [18F]PTBTK3 by JeKo-1 cells in the presence of dimethyl sulfoxide (DMSO) vehicle (n = 3), non-radioactive PTBTK3 (n = 3), or remibrutinib (n = 3).

    Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421.

    Representative PET images at 60 min post injection of U87MG xenografts (n = 3), JeKo-1 xenografts (n = 3), and JeKo-1 xenografts pre-dosed with remibrutinib (0.1 mg, injected intravenously) (n = 3).

    Remibrutinib purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2023 Feb 10;6(3):410-421.

    ROI analysis of tumor uptake in JeKo-1 xenografts (n = 3), U87MG xenografts (n = 3), and JeKo-1 xenografts pre-dosed with remibrutinib (0.1 mg, injected intravenously) (n = 3) at 60 min post injection.

    Remibrutinib purchased from MedChemExpress. Usage Cited in: Blood Adv. 2022 Sep 13;6(17):5049-5060.  [Abstract]

    MOLM-13 grown under normoxic (−) or hypoxic (+) conditions for 24 hours, followed by treatment with gilteritinib (+) alone or in combination with remibrutinib (3 and 5 μM, respectively) for 48 hours. Cell viability was assessed by MTT (n = 4-6). Representative data of three independent experiments.

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    製品説明

    Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2].

    IC50 & Target

    IC50: 1 nM (BTK)[1]
    体外実験

    In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM[1].
    In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC50 value of 0.023 μM, the whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats[1].

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

    Remibrutinib 関連抗体
    臨床実験
    分子量

    507.53

    分子式

    C27H27F2N5O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC(F)=CC(C2=NC=NC(N)=C2OCCN(C)C(C=C)=O)=C1C)C3=CC=C(C4CC4)C=C3F
    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 : 125 mg/mL (246.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9703 mL 9.8516 mL 19.7033 mL
    5 mM 0.3941 mL 1.9703 mL 3.9407 mL
    10 mM 0.1970 mL 0.9852 mL 1.9703 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)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    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）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.76%

    COA (248 KB) HNMR (267 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    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 1.9703 mL 9.8516 mL 19.7033 mL 49.2582 mL
    5 mM 0.3941 mL 1.9703 mL 3.9407 mL 9.8516 mL
    10 mM 0.1970 mL 0.9852 mL 1.9703 mL 4.9258 mL
    15 mM 0.1314 mL 0.6568 mL 1.3136 mL 3.2839 mL
    20 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4629 mL
    25 mM 0.0788 mL 0.3941 mL 0.7881 mL 1.9703 mL
    30 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6419 mL
    40 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2315 mL
    50 mM 0.0394 mL 0.1970 mL 0.3941 mL 0.9852 mL
    60 mM 0.0328 mL 0.1642 mL 0.3284 mL 0.8210 mL
    80 mM 0.0246 mL 0.1231 mL 0.2463 mL 0.6157 mL
    100 mM 0.0197 mL 0.0985 mL 0.1970 mL 0.4926 mL
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    Remibrutinib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    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） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      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:

    Remibrutinib1787294-07-8LOU064LOU 064LOU-064BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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    製品名:
    Remibrutinib
    製品番号:
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