1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. Acalabrutinib

Acalabrutinib  (Synonyms: Calquence; ACP-196)

製品番号: HY-17600 純度: 99.86%
COA 取扱説明書 Technical Support

Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib can be used for CLL research. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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CAS 番号 : 1420477-60-6

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 51 在庫あり
Solution
10 mM * 1 mL in DMSO USD 51 在庫あり
Solid
5 mg $50 在庫あり
10 mg $70 在庫あり
50 mg $130 在庫あり
100 mg $190 在庫あり
200 mg $290 在庫あり
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カスタマーレビュー

Based on 31 publication(s) in Google Scholar

Other Forms of Acalabrutinib:

Top Publications Citing Use of Products

顧客検証

Flow Cytometry
Cell Imaging/Staining
ELISA
Histological Imaging/Staining

    Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199.  [Abstract]

    Aged mice were given vehicle or Acalabrutinib (0.15 mg/mL, drinking water administration) for 21 days (n = 10 per group, pooled from two experiments). Flow cytometry plots; right, FO B cell and ABCs (CD21loCD11c+) percentages among mature B cells.

    Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199.  [Abstract]

    Aged mice were given vehicle or Acalabrutinib (0.15 mg/mL, drinking water administration) for 7 days. Each group was tested in two experiments (n = 4 or 3 per experiment). The percentage of Ki67+ FO B cells and ABCs was compared.

    Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199.  [Abstract]

    Autoantibodies against histone, dsDNA, and Sm/RNP in vehicle- or Acalabrutinib (0.15 mg/mL, drinking water administration, 3 weeks)-treated mice serum were tested by enzyme-linked immunosorbent assay (ELISA). OD, optical density.

    Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199.  [Abstract]

    Representative renal immunostaining of immunoglobulin deposition in kidneys, stained with anti-IgG, and bright-field imaging from vehicle-treated WT and vehicle- or Acalabrutinib (0.15 mg/mL, drinking water administration, 3 weeks)-treated bm12-induced lupus mice. Scale bars, 50 μm.

    Acalabrutinib purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Apr 18;11(16):eadt8199.  [Abstract]

    Schematic for Acalabrutinib treatment from day 0. CD19+ B cells were cultured with R848, IL-21, anti-Ig, and BAFF supplemented with Acalabrutinib (10 μM, 3 days) or DMSO for 3 days. Representative flow cytometry plots of CD11c and T-bet expression in each group on day 3 and the frequency of CD11c+T-bet+ ABCs among live B cells.
    • 生物活性

    • 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

    Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib can be used for CLL research[1][2]. Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target

    IC50: 3 nM (BTK in CD69 B cell)[2]

    Cellular Effect
    Cell Line Type Value Description References
    MOLM-13 IC50
    358 3
    Compound: ACP-196
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    TMD8 IC50
    0.014 1
    Compound: Acalabrutinib
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 33740548]
    NAMALVA IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    MOLM-13 IC50
    358 3
    Compound: ACP-196
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    MOLM-13 IC50
    358 3
    Compound: ACP-196
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Pfeiffer IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    NAMALVA IC50
    >10 3
    Compound: ACP-196
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    NAMALVA IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Raji IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Pfeiffer IC50
    >10 3
    Compound: ACP-196
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Ramos IC50
    31.3 3
    Compound: ACP-196
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Raji IC50
    >10 3
    Compound: ACP-196
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Rec1 IC50
    0.013 3
    Compound: ACP-196
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Ramos IC50
    31.3 3
    Compound: ACP-196
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    SU-DHL-2 IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Rec1 IC50
    0.013 3
    Compound: ACP-196
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    TMD8 IC50
    0.014 1
    Compound: Acalabrutinib
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 33740548]
    SU-DHL-2 IC50
    >10 3
    Compound: ACP-196
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    TMD8 IC50
    0.024 3
    Compound: ACP-196
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    TMD8 IC50
    0.024 3
    Compound: ACP-196
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Pfeiffer IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Raji IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Ramos IC50
    31.3 3
    Compound: ACP-196
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    Rec1 IC50
    0.013 3
    Compound: ACP-196
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    SU-DHL-2 IC50
    > 10 3
    Compound: ACP-196
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    TMD8 IC50
    0.014 1
    Compound: Acalabrutinib
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 33740548]
    TMD8 IC50
    0.024 3
    Compound: ACP-196
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay
    [PMID: 34672559]
    体外実験

    Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation[1].
    Acalabrutinib inhibits purified BTK with an IC50 of 3 nM and an EC50 of 8 nM in a human whole-blood CD69 B cell activation assay. Acalabrutinib has improved target specificity over ibrutinib with 323-, 94-, 19-, and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC , respectively) and no activity against EGFR[2].

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

    体内実験

    Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity[1].

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

    分子量

    465.51

    分子式

    C26H23N7O2

    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light brown

    SMILES

    O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([C@H]5N(C(C#CC)=O)CCC5)=N3)C=C2

    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 : 116.67 mg/mL (250.63 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 2.1482 mL 10.7409 mL 21.4818 mL
    5 mM 0.4296 mL 2.1482 mL 4.2964 mL
    10 mM 0.2148 mL 1.0741 mL 2.1482 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

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    一般には略語で表示されます:C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.47 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 (4.47 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
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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:
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    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: 99.88%

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1482 mL 10.7409 mL 21.4818 mL 53.7045 mL
    5 mM 0.4296 mL 2.1482 mL 4.2964 mL 10.7409 mL
    10 mM 0.2148 mL 1.0741 mL 2.1482 mL 5.3705 mL
    15 mM 0.1432 mL 0.7161 mL 1.4321 mL 3.5803 mL
    20 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
    25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1482 mL
    30 mM 0.0716 mL 0.3580 mL 0.7161 mL 1.7902 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
    80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
    100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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    • Molarity Calculator

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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    Acalabrutinib
    製品番号:
    HY-17600
    数量:
    MCE 日本正規代理店: