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Formula | C26H23N7O2 |
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Molecular Weight | 465.51 | CAS No. | 1420477-60-6 | ||||
Solubility (25°C)* | In vitro | DMSO | 93 mg/mL (199.78 mM) | ||||
Ethanol | 60 mg/mL (128.89 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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 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. acalabrutinib has no effect on EGFR phosphorylation on tyrosine residues Y1068 and Y1173. |
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In vivo | 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]. |
Cell Assay: |
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Data from [Data independently produced by , , BioMed Research International, 2018, Article ID 1023490]
Impact of therapeutic inhibition of oncogenic cell signaling tyrosine kinase on cell metabolism: in vivo-detectable metabolic biomarkers of inhibition [ J Transl Med, 2024, 22(1):622] | PubMed: 38965536 |
BMX controls 3βHSD1 and sex steroid biosynthesis in cancer [ J Clin Invest, 2023, 133(2)e163498] | PubMed: 36647826 |
XPO1 inhibition sensitises CLL cells to NK cell mediated cytotoxicity and overcomes HLA-E expression [ Leukemia, 2023, 10.1038/s41375-023-01984-z] | PubMed: 37528310 |
In Vitro 3D Spheroid Culture System Displays Sustained T Cell-dependent CLL Proliferation and Survival [ Hemasphere, 2023, 7(9):e938] | PubMed: 37637994 |
The Nanomechanical Properties of CLL Cells Are Linked to the Actin Cytoskeleton and Are a Potential Target of BTK Inhibitors [ Hemasphere, 2023, 7(8):e931] | PubMed: 37492437 |
FDA-approved Abl/EGFR/PDGFR kinase inhibitors show potent efficacy against pandemic and seasonal influenza A virus infections of human lung explants [ iScience, 2023, 26(4):106309] | PubMed: 36968089 |
FDA-approved Abl/EGFR/PDGFR kinase inhibitors show potent efficacy against pandemic and seasonal influenza A virus infections of human lung explants [ iScience, 2023, 26(4):106309] | PubMed: 36968089 |
HZ-A-018, a novel inhibitor of Bruton tyrosine kinase, exerts anti-cancer activity and sensitizes 5-FU in gastric cancer cells [ Front Pharmacol, 2023, 14:1142127] | PubMed: 37033615 |
HZ-A-018, a novel inhibitor of Bruton tyrosine kinase, exerts anti-cancer activity and sensitizes 5-FU in gastric cancer cells [ Front Pharmacol, 2023, 14:1142127] | PubMed: 37033615 |
Structure of BTK kinase domain with the second-generation inhibitors acalabrutinib and tirabrutinib [ PLoS One, 2023, 18(8):e0290872] | PubMed: 37651403 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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