Citarinostat (ACY-241)

製品コードS8464 バッチS846401

化学情報

	Synonyms	HDAC-IN-2	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₆ClN₅O₃
	分子量	467.95	CAS No.	1316215-12-9
Solubility (25°C)*	体外	DMSO	93 mg/mL (198.73 mM)
		Ethanol	93 mg/mL (198.73 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
in vitro	In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel also results in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, and is associated with increased frequency of abnormal multipolar mitotic spindle formation, induction of aneuploidy, and increased cell death. In A2780 ovarian cancer cells, 24 hour treatment with 300 nM ACY-241 results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Low exposures of ACY-241 result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes^[1].
in vivo	ACY-241 has a favourable safety profile than non-selective pan-HDAC inhibitors. It has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A2780 ovarian cancer cells
	濃度	0.1, 0.3, 0.5, 1, 3 μM
	反応時間	24 h
	実験の流れ	A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.
動物実験	動物モデル	Female athymic nude mice (Crl:NU(NCr)-Foxn1nu)
	投薬量	50 mg/kg
	投与方法	i.p.

参考

[1] Huang P, et al. Oncotarget. 2017, 8(2):2694-2707.

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：

Overexpression of Human ABCB1 and ABCG2 Reduces the Susceptibility of Cancer Cells to the Histone Deacetylase 6-Specific Inhibitor Citarinostat [ Int J Mol Sci, 2021, 22(5)2592]	PubMed: 33807514
Prolactin Drives a Dynamic STAT5A/HDAC6/HMGN2 Cis-Regulatory Landscape Exploitable in ER+ Breast Cancer [ Endocrinology, 2021, 162(5)bqab036]	PubMed: 33589921
Preclinical validation of Alpha-Enolase (ENO1) as a novel immunometabolic target in multiple myeloma. [ Oncogene, 2020, 39(13):2786-2796]	PubMed: 32024967
Combination of ACY-241 and JQ1 Synergistically Suppresses Metastasis of HNSCC via Regulation of MMP-2 and MMP-9 [ Int J Mol Sci, 2020, 21(18)E6873]	PubMed: 32961679
Selective Inhibition of HDAC6 Sensitizes Cutaneous T-cell Lymphoma to PI3K Inhibitors [ Oncol Lett, 2020, 20(1):533-540]	PubMed: 32565979

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。