Acalabrutinib maleate
Based on 35 publication(s) in Google Scholar
Acalabrutinib (Calquence) maleate 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 maleate demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib maleate can be used for CLL research. Acalabrutinib maleate is a click chemistry reagent, which contains 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.
- CAS No.: 2242394-65-4
- Formula: C30H27N7O6
- Molecular Weight:581.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Acalabrutinib maleate
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]
- Cell Death Dis. 2024 Mar 18;15(3):224. [Abstract]
- Pharmacol Res. 2020 Jan:151:104512. [Abstract]
- Acta Pharmacol Sin. 2021 May;42(5):814-823. [Abstract]
- Int J Biol Macromol. 2019 Apr 15:127:536-543. [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]
- Pharmaceutics. 2022 Sep 5;14(9):1876. [Abstract]
- Biochem Pharmacol. 2026 Mar:245:117660. [Abstract]
- RSC Adv. 2024 May 20;14(23):16170-16193. [Abstract]
- Matrix Biol. 2022 Sep:112:171-189. [Abstract]
- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- Cancers (Basel). 2020 Dec 11;12(12):3731. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Cell Signal. 2022 Aug:96:110358. [Abstract]
- iScience. 2024 Sep 24;27(11):110961. [Abstract]
- Anal Bioanal Chem. 2025 Feb;417(4):821-834. [Abstract]
- Eur J Immunol. 2021 Sep;51(9):2251-2265. [Abstract]
- BMC Cancer. 2021 Jun 26;21(1):732. [Abstract]
- BMC Cancer. 2021 Jun 26;21(1):732.
- ACS Pharmacol Transl Sci. 2025 Mar 12;8(4):917-931. [Abstract]
- Vascul Pharmacol. 2023 Jun:150:107172. [Abstract]
- 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.
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Flow Cytometry
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Cell Imaging/Staining
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ELISA
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Histological Imaging/Staining
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Flow Cytometry
Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2242394-65-4
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Molecular Weight 581.58
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Formula C30H27N7O6
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SMILES
OC(/C=C\C(O)=O)=O.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
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Synonyms
Calquence maleate; ACP-196 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (35)
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Journal Impact Factor
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Most Recent
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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 maleate 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 maleate 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 maleate 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 maleate 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 maleate 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.
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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 -
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 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan:151:104512. PMID: 31726100 -
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 -
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 -
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 -
Pharmaceutics
2022 Sep 5;14(9):1876. PMID: 36145624 -
Biochem Pharmacol
MEK inhibitor induces cardiac complications by preventing ZMYND8-mediated ubiquitination and proteasomal degradation of HMGB1. [Abstract]2026 Mar:245:117660. PMID: 41423035 -
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 -
Matrix Biol
2022 Sep:112:171-189. PMID: 36031013 -
Stem Cell Reports
2019 May 14;12(5):996-1006. PMID: 31031187 -
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 -
Rheumatology (Oxford)
Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]2025 Aug 13:keaf437. PMID: 40802538 -
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 -
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 -
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 -
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 -
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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 -
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 -
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 -
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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 -
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Purity & Documentation
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 SEM, et al. The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia. Clin Cancer Res. 2017 Jun 1;23(11):2831-2841. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)