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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H23N7O2 |
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分子量 | 465.51 | CAS No. | 1420477-60-6 | |
Solubility (25°C)* | 体外 | DMSO | 93 mg/mL (199.78 mM) | |
Ethanol | 93 mg/mL (199.78 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, 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. |
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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. 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]. |
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]. |
細胞アッセイ | 細胞株 | primary human CLL cells,T cells, NK cells, and epithelial cells |
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濃度 | -- | |
反応時間 | -- | |
実験の流れ | -- |
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動物実験 | 動物モデル | canine model of B cell NHL |
投薬量 | 2.5, 5, 10 mg/kg. | |
投与方法 | orally administered |
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Data from [Data independently produced by , , BioMed Research International, 2018, Article ID 1023490]
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 |
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 |
In Vitro 3D Spheroid Culture System Displays Sustained T Cell-dependent CLL Proliferation and Survival [ Hemasphere, 2023, 7(9):e938] | PubMed: 37637994 |
Bruton's TK regulates myeloid cell recruitment during acute inflammation [ Br J Pharmacol, 2022, 179(11):2754-2770] | PubMed: 34897650 |
The Inhibition of Bruton Tyrosine Kinase Alleviates Acute Liver Failure via Downregulation of NLRP3 Inflammasome [ J Immunol, 2022, 209(6):1156-1164] | PubMed: 35977799 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。