Vorinostat (SAHA)

別名：MK0683, Suberoylanilide hydroxamic acid

製品コード：S1047 純度：99.96%

Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.

CAS No. 149647-78-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 28600	国内在庫あり
200mg	JPY 22000	国内在庫あり
500mg	JPY 33000	国内在庫あり
2g	JPY 73500	国内在庫あり
10g	JPY 220500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

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製品安全説明書

現在のバッチを見る：純度： 99.96%

99.96

Vorinostat (SAHA)関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HCT116	Apoptosis Assay	3 μM	24 h	does not induce apoptosis assessed as increase in p53 protein level	24766560
Jurkat	Cytotoxic Assay	20 μM	72 h	no cytotoxicity assessed as growth inhibition	24304348
MDA-MB-231	Kinase Assay	1 μM	24 h	does not inhibit HDAC6 assessed as acetylation levels of tubulin	23493449
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生物活性

製品説明

Vorinostat (SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.

Targets

HDAC ^[1]
(Cell-free assay)

~10 nM

In Vitro
In vitro	Vorinostat inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively. Vorinostat also results in a marked hyperacetylation of histone H4. ^[1] Vorinostat inhibits the growth of three prostate cancer cell lines LNCaP, PC-3 and TSU-Pr1 at micromolar concentrations (2.5-7.5 μM), and induces dose-dependent cell death in LNCaP cells. ^[2] Vorinostat treatment in MCF-7 cells inhibits cell proliferation at an IC50 of 0.75 μM resulting in the accumulation of cells in the G1 and G2-M phase of the cell cycle. Vorinostat also induces differentiation in the estrogen receptor-negative cell line SKBr-3 and the retinoblastoma-negative cell line MDA-468. ^[3] Vorinostat treatment at 1 μM for 8 hours or more is sufficient to irreversibly induce apoptosis of human multiple myeloma (MM) cells. The gene expression profiles of Vorinostat treated MM cells are not hallmarked by global transcriptional activation, but by coordinated transcriptional changes of specific functional groups of genes such as cytokine-induced proliferative/survival signaling cascades, oncogenes-tumor suppressor genes, regulators of apoptosis, DNA synthesis-repair and cell cycle, and proteasome-ubiquitin function. ^[4]
Kinase Assay	Immunoprecipitation-HDAC assays
Kinase Assay	The lysate of Jurkat cells is incubated for 1 hour on ice and cleared by centrifugation at 12,000 g for 10 minutes at 4 °C. Supernatants are precleared with 30 μL of 50% protein G-Sepharose slurry for 1 hour at 4 °C. Beads are pelleted by centrifugation and supernatants are incubated for 1 hour at 4 °C with 10 μg of IgG fraction from anti-HDAC1 or HDAC3 polyclonal antisera (preincubated 2 hours at room temperature with either the homologous or heterologous immunizing peptide). Both antisera are raised in rabbits against the carboxylterminal peptide of HDAC1 and HDAC3 by using synthetic peptides coupled to keyhole limpet hemocyanin. 30 μL of 50% protein G-Sepharose slurry is added for 1 hour at 4 °C. Immune complexes are pelleted by centrifugation and washed three times with 1 mL of lysis buffer. Beads are resuspended in 200 μL of HDAC buffer (20 mM Tris-HCl, pH 8.0/150 mM NaCl/10% glycerol), and the HDAC assay is performed with an ³H-acetylated peptide corresponding to amino acids 1-24 of histone H4. Released [³H]acetic acid is quantified by scintillation counting. For inhibitions studies, the immunoprecipitated complexes are preincubated with the different concentrations of Vorinostat for 30 minutes at 4 °C.
細胞実験	細胞株	LNCaP, PC-3, and TSU-Pr1
	濃度	Dissolved in DMSO, final concentrations ~7.5 μM
	反応時間	1, 2, 3 and 4 days
	実験の流れ	Cells are exposed to various concentrations of Vorinostat for 1, 2, 3 and 4 days. Cell viability is assessed by trypan blue dye exclusion.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	Ac-Histone H4 / Ac-Histone H3 phospho-CDK1 phospho-Cdc25c / Cdc25c Cyclin B1 c-Myc / c-Raf / Akt / Cyclin D1 / CDK4 p-eIF2α / ATF4 / CHOP p21		21598070
	Immunofluorescence	HDAC1 / CK19 Nrf2 α-SMA Ac-STAT3 / IGF2		29917299
	Growth inhibition assay	Cell apoptosis Cell viability		19440035
	ELISA	IGF2 IL-13 / IL-10 / IL-5 M-CSF MMP-9		27086926

In Vivo
In Vivo	Administration of Vorinostat (~100 mg/kg/day) significantly inhibits the growth of CWR22 human prostate xenografts in nude mice with tumor reductions of 78%, 97% and 97%, at doses of 25 mg/kg/day, 50 mg/kg/day and 100 mg/kg/day, respectively, compared with control. Vorinostat induces the accumulation of acetylated core histones and prostate-specific antigen mRNA expression in CWR22 cells, resulting in higher levels of serum prostate-specific antigen than predicted from tumor volume alone. ^[2] Oral administration of Vorinostat (0.67g/L) crosses the blood-brain barrier, increases histone acetylation in the brain, and dramatically improves the motor impairment in the R6/2 mice model of Huntington's disease. ^[5]
動物実験	動物モデル	Male BALB/c nude (nu/nu) mice implanted with CWR22 tumor cells
	投与量	25, 50, and 100 mg/kg/day
	投与経路	Injection i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05700630	Withdrawn	HIV-1-infection\|ART\|Cd4+ Lymphocyte Deficiency\|Lymphoid Tissue; Infection\|Interleukin	Masonic Cancer Center University of Minnesota	July 15 2024	Phase 1
NCT03022565	Withdrawn	Uveal Melanoma	University of Miami\|University of Miami Sylvester Comprehensive Cancer Center	January 2020	Early Phase 1
NCT03167437	Recruiting	Crohn''s Disease	National Institute of Allergy and Infectious Diseases (NIAID)\|National Institutes of Health Clinical Center (CC)	October 30 2017	Phase 1\|Phase 2
NCT03056495	Terminated	Alzheimer Disease	German Center for Neurodegenerative Diseases (DZNE)\|University Hospital Bonn\|University of Göttingen	September 28 2017	Phase 1

参考
[1] Richon VM, et al. Proc Natl Acad Sci U S A, 1998, 95(6), 3003-3007. [2] Butler LM, et al. Cancer Res, 2000, 60(18), 5165-5170. [3] Munster PN, et al. Cancer Res, 2001, 61(23), 8492-8497. [4] Hockly E, et al. Natl Acad Sci U S A, 2003, 100(4), 2041-2046. [5] Mitsiades CS, et al. Proc Natl Acad Sci U S A, 2004, 101(2), 540-545. [6] Pei XY, et al. Clin Cancer Res, 2004, 10(11), 3839-3852. [7] Zhang G, et al. Clin Cancer Res, 2008, 14(17), 5385-5399. [8] Dai Y, et al. Blood, 2008, 112(3), 793-804. + 展開

参考

+ 展開

化学情報

分子量	264.3	化学式	C₁₄H₂₀N₂O₃
CAS No.	149647-78-9	SDF	Download Vorinostat (SAHA) SDFをダウンロードする
Smiles	C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 52 mg/mL ( (196.74 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 6.5 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

Clear solution

5%DMSO 1 Corn oil

2.5mg/ml (9.46mM)

Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
What’s the recommendation about reconstitution of the compound for in vivo animal study?

回答
We recommend the following vehicle for S1047: 2% DMSO, 40% PEG 300, 5% Propylene glycol, 1% Tween 80 at 5 mg/mL.

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C5=C4/X	C5:	LOG(C5):
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