Acalabrutinib (ACP-196)
For research use only.
Catalog No.S8116
16 publications

CAS No. 1420477-60-6
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.
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Comparison of the impairment of ADCC against primary CLL cells by different irreversible BTK inhibitors. The antibody-dependent increase in the percentages of minimal calcein retention was determined with 3-fold excess of 1708-LC3E11 effector cells over CLL target cells in seven independent experiments. (a) Asterisks above the boxes and whiskers denote the significance of enhanced cytotoxicity compared to the control without addition of antibodies and inhibitors as determined by paired t-tests. Furthermore combination treatment was compared to that with anti-CD20 antibodies as single agents. (b) The mean differences ± SEM in the cytotoxicity against CLL cells in the presence and absence of rituximab and obinutuzumab were calculated from the data shown in (a). The ADCC of rituximab and obinutuzumab was compared by paired two-tailed t-test. *p<0.05; **p<0.01; ***p<0.001.
BioMed Research International, 2018, Article ID 1023490. Acalabrutinib (ACP-196) purchased from Selleck.
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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. | |||||||||||||||||||||||
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Targets |
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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]. |
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Cell Data |
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Assay |
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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]. |
Protocol
Cell Research: |
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Animal Research: |
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Solubility (25°C)
In vitro | DMSO | 93 mg/mL (199.78 mM) |
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Ethanol | 93 mg/mL (199.78 mM) | |
Water | Insoluble | |
In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing. |
6mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
Molecular Weight | 465.51 |
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Formula | C26H23N7O2 |
CAS No. | 1420477-60-6 |
Storage |
powder in solvent |
Synonyms | N/A |
Smiles | CC#CC(=O)N1CCCC1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5 |
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
Dosage | mg/kg | Average weight of animals | g | Dosing volume per animal | ul | Number of animals | ||||
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% DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
Method for preparing in vivo formulation:Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80,mix and clarify, next add μL ddH2O,mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT04688151 | Not yet recruiting | Drug: Rituximab | Primary Central Nervous System Lymphoma (PCNSL) | National Health Research Institutes Taiwan|National Taiwan University Hospital|National Cheng-Kung University Hospital|China Medical University Hospital|Chang Gung Memorial Hospital | February 1 2021 | Phase 1 |
NCT04660045 | Not yet recruiting | Drug: Acalabrutinib | Chronic Lymphocytic Leukemia|CLL/SLL | Weill Medical College of Cornell University|AstraZeneca | January 2021 | Phase 2 |
NCT04657094 | Recruiting | Drug: Acalabrutinib | Autoimmune Hemolytic Anemia|Chronic Lymphocytic Leukemia|Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma|Warm Antibody Autoimmune Hemolytic Anemia | City of Hope Medical Center|National Cancer Institute (NCI) | January 20 2021 | Phase 2 |
NCT04523428 | Not yet recruiting | Drug: Venetoclax/Acalabrutinib | CLL/SLL | Stichting Hemato-Oncologie voor Volwassenen Nederland | December 2020 | Phase 2 |
NCT04502394 | Recruiting | Drug: KRT-232|Drug: acalabrutinib | Diffuse Large B Cell Lymphoma|Chronic Lymphocytic Leukemia|Non Hodgkin Lymphoma | Kartos Therapeutics Inc. | December 2020 | Phase 1|Phase 2 |
NCT04630756 | Recruiting | Drug: AZD4573|Drug: Acalabrutinib | Advanced Haematological Malignancies | AstraZeneca|Parexel | December 17 2020 | Phase 1|Phase 2 |
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