Home Angiogenesis BTK inhibitor Acalabrutinib (ACP-196) For research use only.

Acalabrutinib (ACP-196)

Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 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.

Acalabrutinib (ACP-196) Chemical Structure

Acalabrutinib (ACP-196) Chemical Structure

CAS: 1420477-60-6

Selleck's Acalabrutinib (ACP-196) has been cited by 43 publications

Purity & Quality Control

Batch: Purity: 99.89%
99.89

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CLL cells Apoptosis assay 1 μM or 3 μM 24, 48 and 72 h increases in apoptosis rates in primary CLL cells at 24, 48, and 72 hours of treatment 28034907
B cells Function assay 1 hr Inhibition of BTK in human whole blood-derived CD19+ B cells assessed as suppression of anti-IgM stimulated-CD69 expression preincubated for 1 hr followed by IgM stimulation for 18 hrs by FACS analysis, IC50 = 0.198 μM. 29457982
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Biological Activity

Description Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 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.
Targets
BTK [1]
(in a human whole-blood CD69 B cell activation assay)
3nM
In vitro
In vitro In the in vitro signaling assay on primary human CLL cells, acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT. Acalabrutinib demonstrates higher selectivity for BTK with IC50 determinations on nine kinases with a cysteine residue in the same position as BTK. Importantly, unlike ibrutinib, acalabrutinib does not inhibit EGFR, ITK, or TEC. acalabrutinib has no effect on EGFR phosphorylation on tyrosine residues Y1068 and Y1173. Compared with ibrutinib, acalabrutinib has much higher IC50(>1000 nM) or virtually no inhibition on kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1[1].
Cell Research Cell lines primary human CLL cells,T cells, NK cells, and epithelial cells
Concentrations --
Incubation Time --
Method

--
Experimental Result Images Methods Biomarkers Images PMID
Western blot pBTK / BTK / pAKT / AKT / pERK / ERK / pS6 / S6 28034907
In Vivo
In vivo oral administration of ACP-196 in mice results in dose-dependent inhibition of anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34 mg/kg compared to 0.91 mg/kg for ibrutinib. A similar model is used to compare the duration of Btk inhibition after a single oral dose of 25 mg/kg. ACP-196 inhibits CD86 expression >90% at 3h postdose[3].
Animal Research Animal Models canine model of B cell NHL
Dosages 2.5, 5, 10 mg/kg.
Administration orally administered 
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06170671 Recruiting Chronic Lymphocytic Leukemia AstraZeneca December 13 2023 --
NCT05951959 Not yet recruiting Mantle Cell Lymphoma (MCL) AstraZeneca November 9 2023 Phase 2
NCT05999877 Recruiting Chronic Lymphocytic Leukemia AstraZeneca July 11 2023 --
NCT05820841 Recruiting Large B-cell Lymphoma|Diffuse Large B Cell Lymphoma Universität des Saarlandes|University of Leipzig|University Hospital Regensburg|Wuerzburg University Hospital|University Hospital of Gießen and Marburg|Saarland University Medical Center|AstraZeneca June 7 2023 Phase 3
NCT05256641 Recruiting Diffuse Large B-Cell Lymphoma|High-grade B-cell Lymphoma|Transformed Lymphoma|Secondary Central Nervous System Lymphoma Jonsson Comprehensive Cancer Center|AstraZeneca January 23 2023 Phase 1|Phase 2
NCT05557695 Recruiting Chronic Lymphocytic Leukemia CLL AstraZeneca|UKCLL Forum October 17 2022 --

Chemical lnformation & Solubility

Molecular Weight 465.51 Formula

C26H23N7O2
CAS No. 1420477-60-6 SDF Download Acalabrutinib (ACP-196) SDF
Smiles CC#CC(=O)N1CCCC1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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