Acalabrutinib (ACP-196)

製品コードS8116 バッチS811602

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₆H₂₃N₇O₂

分子量

465.51

CAS No.

1420477-60-6

Solubility (25°C)*

体外

DMSO

93 mg/mL (199.78 mM)

Ethanol

60 mg/mL (128.89 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

2% DMSO 1 30% PEG 300 2 2%Tween80 3 66%ddH2O

1.5mg/ml

Taking the 1 mL working solution as an example, add 20 μL of 75 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	primary human CLL cells,T cells, NK cells, and epithelial cells
	濃度	--
	反応時間	--
	実験の流れ	--
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

参考

カスタマーフィードバック

: Data from [Data independently produced by , , BioMed Research International, 2018, Article ID 1023490]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。