For research use only.
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.
Selleck's Acalabrutinib (ACP-196) has been cited by 19 publications
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|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.|
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.
|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.|
|In vitro||DMSO||93 mg/mL (199.78 mM)|
|Ethanol||93 mg/mL (199.78 mM)|
|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.
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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|
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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)||June 30 2021||Phase 2|
|NCT04660045||Not yet recruiting||Drug: Acalabrutinib||Chronic Lymphocytic Leukemia|CLL/SLL||Weill Medical College of Cornell University|AstraZeneca||May 2021||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|
|NCT04867980||Completed||Drug: ACP-196|Drug: Moxifloxacin 400 mg|Drug: Placebo||Healthy Volunteers||Acerta Pharma BV||April 1 2016||Phase 1|
|NCT04876807||Completed||Drug: ACP-196|Drug: Omeprazole||Healthy Volunteers||Acerta Pharma BV||January 28 2016||Phase 1|
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.
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