Acalabrutinib
Based on 35 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 1420477-60-6
- Formula: C26H23N7O2
- Molecular Weight:465.51
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Acalabrutinib
More- Signal Transduct Target Ther. 2020 Sep 14;5(1):200. [Abstract]
- Sci Adv. 2025 Apr 18;11(16):eadt8199. [Abstract]
- Blood Cancer J. 2026 May 7;16(1):107. [Abstract]
- Pharmacol Res. 2020 Jan;151:104512. [Abstract]
- Cell Death Dis. 2024 Mar 18;15(3):224. [Abstract]
- Int J Biol Macromol. 2019 Apr 15:127:536-543. [Abstract]
- Acta Pharmacol Sin. 2021 May;42(5):814-823. [Abstract]
- Blood Adv. 2026 Jun 5:bloodadvances.2025019077. [Abstract]
- J Med Chem. 2021 Nov 11;64(21):16242-16270. [Abstract]
- J Med Chem. 2019 Jul 25;62(14):6561-6574. [Abstract]
- Biochem Pharmacol. 2025 Dec 19:245:117660. [Abstract]
- Pharmaceutics. 2022 Sep 5;14(9):1876. [Abstract]
- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- Matrix Biol. 2022 Sep:112:171-189. [Abstract]
- RSC Adv. 2024 May 20;14(23):16170-16193. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Cancers (Basel). 2020 Dec 11;12(12):3731. [Abstract]
- iScience. 2024 Sep 24;27(11):110961. [Abstract]
- Anal Bioanal Chem. 2025 Feb;417(4):821-834. [Abstract]
- ACS Pharmacol Transl Sci. 2025 Mar 12;8(4):917-931. [Abstract]
- Cell Signal. 2022 Aug:96:110358. [Abstract]
- Eur J Immunol. 2021 Sep;51(9):2251-2265. [Abstract]
- Vascul Pharmacol. 2023 Jun:150:107172. [Abstract]
- BMC Cancer. 2021 Jun 26;21(1):732. [Abstract]
- BMC Cancer. 2021 Jun 26;21(1):732.
- Front Cardiovasc Med. 2023 Aug 15:10:1190099. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- bioRxiv. 2026 May 8:2026.05.07.723540. [Abstract]
- Patent. US20250295655A1.
- bioRxiv. 2025 April 24.
- bioRxiv. 2024 September 08.
- bioRxiv. 2024 Oct 10:2023.12.18.572223. [Abstract]
- bioRxiv. 2023 Jul 29.
- bioRxiv. 2023 Feb 24.
-
Flow Cytometry
-
Cell Imaging/Staining
-
ELISA
-
Histological Imaging/Staining
-
Flow Cytometry
Biological Activity
IC50: 3 nM (BTK in CD69 B cell)[2]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
358 μM
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] |
| NAMALVA | IC50 |
>10 μM
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] |
| Pfeiffer | IC50 |
>10 μM
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 μM
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 μM
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 μM
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 μM
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 nM
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 μM
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1420477-60-6
-
Appearance Solid
-
Molecular Weight 465.51
-
Formula C26H23N7O2
-
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
-
Synonyms
Calquence; ACP-196
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (35)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Discovery of a highly potent and selective Bruton's tyrosine kinase inhibitor avoiding impairment of ADCC effects for B-cell non-Hodgkin lymphoma. [Abstract]2020 Sep 14;5(1):200. PMID: 32929063 -
Sci Adv
Critical roles of chronic BCR signaling in the differentiation of anergic B cells into age-associated B cells in aging and autoimmunity. [Abstract]2025 Apr 18;11(16):eadt8199. PMID: 40249819
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.
-
Blood Cancer J
Docirbrutinib is a pan-mutant BTK inhibitor and inhibits B-cell receptor signaling in chronic lymphocytic leukemia cells in preclinical and early clinical investigations. [Abstract]2026 May 7;16(1):107. PMID: 42098067 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan;151:104512. PMID: 31726100 -
Cell Death Dis
Disrupting pro-survival and inflammatory pathways with dimethyl fumarate sensitizes chronic lymphocytic leukemia to cell death. [Abstract]2024 Mar 18;15(3):224. PMID: 38494482 -
Int J Biol Macromol
Novel BTK inhibitor acalabrutinib (ACP-196) tightly binds to site I of the human serum albumin as observed by spectroscopic and computational studies. [Abstract]2019 Apr 15:127:536-543. PMID: 30664965 -
Acta Pharmacol Sin
Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma. [Abstract]2021 May;42(5):814-823. PMID: 32855532 -
Blood Adv
PLCG2 Exon-Skipped Variants: Insights into Their Potential Role in Chronic Lymphocytic Leukemia. [Abstract]2026 Jun 5:bloodadvances.2025019077. PMID: 42263669 -
J Med Chem
Discovery of 1-Amino-1 H-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors. [Abstract]2021 Nov 11;64(21):16242-16270. PMID: 34672559 -
J Med Chem
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis. [Abstract]2019 Jul 25;62(14):6561-6574. PMID: 31260299 -
Biochem Pharmacol
MEK inhibitor induces cardiac complications by preventing ZMYND8-mediated ubiquitination and proteasomal degradation of HMGB1. [Abstract]2025 Dec 19:245:117660. PMID: 41423035 -
Pharmaceutics
2022 Sep 5;14(9):1876. PMID: 36145624 -
Stem Cell Reports
2019 May 14;12(5):996-1006. PMID: 31031187 -
Matrix Biol
2022 Sep:112:171-189. PMID: 36031013 -
RSC Adv
Ion Trap LC/MS reveals the generation of reactive intermediates in acalabrutinib metabolism: phase I metabolic profiling and bioactivation pathways elucidation. [Abstract]2024 May 20;14(23):16170-16193. PMID: 38769961 -
Rheumatology (Oxford)
Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]2025 Aug 13:keaf437. PMID: 40802538 -
Cancers (Basel)
Bruton's Tyrosine Kinase Inhibitors Ibrutinib and Acalabrutinib Counteract Anthracycline Resistance in Cancer Cells Expressing AKR1C3. [Abstract]2020 Dec 11;12(12):3731. PMID: 33322571 -
iScience
Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]2024 Sep 24;27(11):110961. PMID: 39759071 -
Anal Bioanal Chem
Development, validation, and clinical application of LC-MS/MS method for simultaneous determination of ibrutinib, zanubrutinib, orelabrutinib, acalabrutinib, and their active metabolites in patients with B-cell lymphoma. [Abstract]2025 Feb;417(4):821-834. PMID: 39702674 -
ACS Pharmacol Transl Sci
Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]2025 Mar 12;8(4):917-931. PMID: 40242575 -
Cell Signal
BTK-independent regulation of calcium signalling downstream of the B-cell receptor in malignant B-cells. [Abstract]2022 Aug:96:110358. PMID: 35597428 -
Eur J Immunol
Bruton's tyrosine kinase inhibition induces rewiring of proximal and distal B-cell receptor signaling in mice. [Abstract]2021 Sep;51(9):2251-2265. PMID: 34323286 -
Vascul Pharmacol
Bruton's Tyrosine Kinase inhibition by Acalabrutinib does not affect early or advanced atherosclerotic plaque size and morphology in Ldlr-/- mice. [Abstract]2023 Jun:150:107172. PMID: 37075932 -
BMC Cancer
Distinct BTK inhibitors differentially induce apoptosis but similarly suppress chemotaxis and lipid accumulation in mantle cell lymphoma. [Abstract]2021 Jun 26;21(1):732. PMID: 34174847 -
-
Front Cardiovasc Med
Ibrutinib impairs IGF-1-dependent activation of intracellular Ca handling in isolated mouse ventricular myocytes. [Abstract]2023 Aug 15:10:1190099. PMID: 37655217 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
bioRxiv
More than an attachment module: covalent inhibitor warheads influence BTK dynamics and function. [Abstract]2026 May 8:2026.05.07.723540. PMID: 42146433 -
-
-
-
bioRxiv
Impact of the clinically approved BTK inhibitors on the conformation of full-length BTK and analysis of the development of BTK resistance mutations in chronic lymphocytic leukemia. [Abstract]2024 Oct 10:2023.12.18.572223. PMID: 38187560 -
-
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
-
Handling Instructions (2659 KB)
References
[1]. Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21 [Content Brief]
[2]. Herman SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 30 [Content Brief]
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 |