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Acalabrutinib

Alias ACP-196
Acalabrutinib

Acalabrutinib

Product Introduction

Bioactivity
Description
Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
Targets&IC50
BTK:3nM
In vitro
When administered orally to mice, ACP-196 demonstrably inhibits the expression of CD86 in CD19+ spleen cells induced by anti-IgM in a dose-dependent manner, with an ED50 of 0.34 mg/kg. This inhibition exceeded 90% of CD86 expression levels after 3 hours post-treatment.
In vivo
Acalabrutinib does not inhibit EGFR, ITK, and TEC, and does not affect the phosphorylation of EGFR at the Y1068 and Y1173 sites. It has a higher IC50 value than ibrutinib and shows almost no inhibitory activity on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In in vitro signal detection in primary human chronic lymphocytic leukemia cells, Acalabrutinib inhibits the tyrosine phosphorylation of downstream targets ERK, IKB, and AKT.
AliasACP-196
Chemical Properties
Molecular Weight465.51
FormulaC26H23N7O2
Cas No.1420477-60-6
SmilesCC#CC(=O)N1CCC[C@H]1c1nc(-c2ccc(cc2)C(=O)Nc2ccccn2)c2c(N)nccn12
Relative Density.1.37 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: 53 mg/mL (113.9 mM)
DMSO: 86 mg/mL (184.7 mM)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.1482 mL10.7409 mL21.4818 mL107.4091 mL
5 mM0.4296 mL2.1482 mL4.2964 mL21.4818 mL
10 mM0.2148 mL1.0741 mL2.1482 mL10.7409 mL
20 mM0.1074 mL0.5370 mL1.0741 mL5.3705 mL
50 mM0.0430 mL0.2148 mL0.4296 mL2.1482 mL
100 mM0.0215 mL0.1074 mL0.2148 mL1.0741 mL