Home Angiogenesis BTK inhibitor Acalabrutinib (ACP-196)

Acalabrutinib (ACP-196)

Catalog No.S8116

For research use only.

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

CAS No. 1420477-60-6

Selleck's Acalabrutinib (ACP-196) has been cited by 32 publications

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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 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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CLL cells M3TvN2Fxd3C2b4Ppd{Bie3OjeR?= NHfEO2EyKM7:TTDvdkA{KM7:TR?= M1S2OVI1NCB2ODDhcoQhPzJiaB?= MnT4bY5kemWjc3XzJIlvKGGyb4D0c5NqeyC{YYTld{BqdiCycnntZZJ6KEOOTDDj[YxteyCjdDCyOEwhPDhuIHHu[EA4OiCqb4Xyd{Bw\iC2cnXheI1mdnR? Ml7kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyM{S5NFcoRjJ6MEO0PVA4RC:jPh?=
B cells MVLGeY5kfGmxbjDhd5NigQ>? MlL3NUBpeg>? NUXXPFhbUW6qaXLpeIlwdiCxZjDCWGshcW5iaIXtZY4hf2ixbHWgZoxwd2RvZHXybZZm\CCFREG5L{BDKGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJIFvfGlvSXfNJJN1cW23bHH0[YQuS0R4OTDlfJBz\XO|aX;uJJBz\WmwY4XiZZRm\CCob4KgNUBpeiCob3zsc5dm\CCkeTDJ[20he3SrbYXsZZRqd25iZn;yJFE5KGi{czDifUBHSUOVIHHuZYx6e2m|LDDJR|UxKD1iMD6xPVgh|ryPLh?= MlnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2NUe5PFIoRjJ7NEW3PVgzRC:jPh?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot pBTK / BTK / pAKT / AKT / pERK / ERK / pS6 / S6 28034907
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 (from reference)

Cell Research:

[1]
  • Cell lines: primary human CLL cells,T cells, NK cells, and epithelial cells
  • Concentrations: --
  • Incubation Time: --
  • Method:

    --
Animal Research:

[2]
  • Animal Models: canine model of B cell NHL
  • Dosages: 2.5, 5, 10 mg/kg.
  • Administration: orally administered 

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 465.51
Formula

C26H23N7O2
CAS No. 1420477-60-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC#CC(=O)N1CCCC1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5

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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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05256641 Not yet recruiting Drug: Acalabrutinib Diffuse Large B-Cell Lymphoma|High-grade B-cell Lymphoma|Transformed Lymphoma|Secondary Central Nervous System Lymphoma Jonsson Comprehensive Cancer Center|AstraZeneca September 1 2022 Phase 1|Phase 2
NCT05437250 Not yet recruiting Drug: Non interventional study Chronic Lymphocytic Leukemia AstraZeneca July 15 2022 --
NCT04660045 Withdrawn Drug: Acalabrutinib Chronic Lymphocytic Leukemia|CLL/SLL Weill Medical College of Cornell University|AstraZeneca May 2022 Phase 2
NCT05038904 Recruiting Drug: Acalabrutinib Food Allergy|Food Allergy Peanut Johns Hopkins University|AstraZeneca December 16 2021 Phase 2
NCT04546620 Recruiting Drug: R-CHOP|Drug: R-CHOP + acalabrutinib Diffuse Large B Cell Lymphoma University Hospital Southampton NHS Foundation Trust|AstraZeneca October 19 2021 Phase 2
NCT04963946 Recruiting Drug: Stop ACA|Drug: ACA Continuation Untreated Chronic Lymphocytic Leukemia French Innovative Leukemia Organisation October 18 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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