Acalabrutinib (ACP-196)

製品コードS8116 バッチS811603

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

93 mg/mL (199.78 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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 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 an in vitro signaling assay on primary human CLL cells, Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT. It demonstrates higher selectivity for BTK with IC50 determinations on nine kinases with a cysteine residue in the same position as BTK. This compound has no effect on EGFR phosphorylation on tyrosine residues Y1068 and Y1173.
in vivo	A similar model is used to compare the duration of Btk inhibition after a single oral dose of 25 mg/kg of Acalabrutinib (ACP-196). It 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

https://pubmed.ncbi.nlm.nih.gov/26957112/
http://cancerres.aacrjournals.org/content/74/19_Supplement/1744
http://cancerres.aacrjournals.org/content/75/15_Supplement/2596

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：

Bruton's tyrosine kinase (BTK) and matrix metalloproteinase-9 (MMP-9) regulate NLRP3 inflammasome-dependent cytokine and neutrophil extracellular trap responses in primary neutrophils [ J Allergy Clin Immunol, 2025, 155(2):569-582]	PubMed: 39547282
A Triple Oral Combination of Bendamustine, Acalabrutinib, and Venetoclax Demonstrates Efficacy Against Mantle Cell Lymphoma In Vitro and In Vivo [ Cancers (Basel), 2025, 17(11)1889]	PubMed: 40507368
Integrating Single-Cell Biophysical and Transcriptomic Features to Resolve Functional Heterogeneity in Mantle Cell Lymphoma [ bioRxiv, 2025, 2025.05.20.655210]	PubMed: 40475412
FoxO1/Rictor axis induces a nongenetic adaptation to ibrutinib via Akt activation in chronic lymphocytic leukemia [ J Clin Invest, 2024, 134(23)e173770]	PubMed: 39436708
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
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Targeting N-linked Glycosylation for the Therapy of Aggressive Lymphomas [ Cancer Discov, 2023, 13(8):1862-1883]	PubMed: 37141112
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

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。