Fig. 1 · Structure

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Acalabrutinib (ACP-196)

Cat. No. A15824 CAS 1420477-60-6

Btk Inhibitor

ACP-196 is an orally available inhibitor of Bruton–s tyrosine kinase (BTK) with potential antineoplastic activity. It inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway.

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Biological Activity

Target & Activity

Target Activity Value
BTK 3nM

Cellular Effect

Cell Line Activity Value Description Reference
MOLM-13 IC50 358 μM Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
NAMALVA IC50 > 10 μM Antiproliferative activity against human NAMALWA cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
Pfeiffer IC50 > 10 μM Antiproliferative activity against human Pfeiffer cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
Raji IC50 > 10 μM Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
Ramos IC50 31.3 μM Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
Rec1 IC50 0.013 μM Antiproliferative activity against human REC-1 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
SU-DHL-2 IC50 > 10 μM Antiproliferative activity against human SUDHL2 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]
TMD8 IC50 0.014 nM Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay [PMID: 33740548]
TMD8 IC50 0.024 μM Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay [PMID: 34672559]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1420477-60-6
Applications Btk Inhibitor
Formula C26H23N7O2
Molecular Weight 465.52
Synonyms ACP196
SMILES
CC#CC(=O)N1CCCC1C2=NC(=C3N2C=CN=C3N)C4=CC=C(C=C4)C(=O)NC5=CC=CC=N5

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 80 mg/mL (171.85 mM)
Water Insoluble
Ethanol 80 mg/mL (171.85 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
5 mg/mL
Vehicle
2% DMSO+30% PEG 300+2% Tween 80+ddH2O

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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