Pracinostat (SB939)

製品コード：S1515 純度：99.99%

Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.

CAS No. 929016-96-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 45000	国内在庫あり
5mg	JPY 31500	国内在庫あり
10mg	JPY 55500	国内在庫あり
50mg	JPY 130500	国内在庫あり
200mg	JPY 220500	国内在庫なし(納期7~10日)
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（23）

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製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Pracinostat (SB939)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 Angiogenesis Related compound Library TGF-beta/Smad compound library Cytoskeletal Signaling Pathway Compound Library Anti-Cardiovascular Disease Compound 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	Incubation Time	活性情報	PMID
MDA-MB-435 cells	Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.48 μM	24119555
HCT116 cells	Proliferation assay	48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.24 μM	24119555
NCI-H460 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.22 μM	24119555
MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.17 μM	24119555
OVCAR5 cells	Proliferation assay	48 h	Antiproliferative activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=0.61 μM	24119555
HepG2	Antiplasmodial assay	53 hrs	Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells after 53 hrs by DAPI staining-based method, IC50 = 0.15 μM.	28241112
Sf9	Function assay	2 hrs	Inhibition of recombinant human HDAC-2 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
HEK293-F	Function assay	2 hrs	Inhibition of recombinant human HDAC-8 expressed in HEK293-F cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
Sf9	Function assay	2 hrs	Inhibition of recombinant human HDAC-1 expressed in baculovirus infected insect Sf9 cells using Fluor de Lys as substrate preincubated for 2 hrs followed by substrate addition measured after 10 mins by fluorescence assay, Ki = 0.016 μM.	ChEMBL
HepG2	Antimalarial assay		Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells, IC50 = 0.15 μM.	24904967
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生物活性

製品説明

特性

A new histone deacetylase inhibitor based on hydroxamic acid, with improved physicochemical, pharmaceutical, and pharmacokinetic properties.

Targets

HDAC10 ^[1] (Cell-free assay)	HDAC3 ^[1] (Cell-free assay)	HDAC5 ^[1] (Cell-free assay)	HDAC1 ^[1] (Cell-free assay)	HDAC4 ^[1] (Cell-free assay)	もっとクリックする
40 nM	43 nM	47 nM	49 nM	56 nM	もっとクリックする

In Vitro
In vitro	SB939 has a 100-fold greater selectivity for HDACs than for Zn-binding non-HDAC enzymes, receptors, and ion channels. SB939 is a potent inhibitor of HDAC class I isoenzymes, HDAC1, HDAC2, HDAC3 and HDAC8 with the IC50 values ranging from 43 nM to 140 nM. SB939 inhibits HDAC class II isoenzymes , HDAC4, HDAC5, HDAC7, HDAC9 and HDAC10 significantly with the IC50 values ranging from 40 nM to 137 nM, with the exception of HDAC6 which shows IC50 of 1008 nM. It markedly inhibits HDAC11 of the HDAC class IV enzymes with IC50 of 93 nM, but shows no inhibitory activity against SIRT 1 of the class III HDACs. SB939 shows significant antiproliferative activity against a wide variety of tumor cell lines, especially Leukemia cells and cutaneous T-cell Lymphoma cells with IC50 values ranging from 50 nM (H9 cells) to 170 nM (HEL92.1.7 cells). ^[1]
Kinase Assay	HDAC enzyme assay
Kinase Assay	All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl₂ and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software.
細胞実験	細胞株	HCT116, A2780, ACHN, MCF7, HL-60, et al.
	濃度	Dissolved in DMSO (stock concentration, 10 mM), final concentrations 1.5 nM to 100 μM
	反応時間	96 hours
	実験の流れ	Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-JAK2 / JAK2 / p-STAT5 / STAT5 / p-FLT3 / FLT3		22829971

In Vivo
In Vivo	Administration of SB939 (25 mg/kg to 100 mg/kg) displays a dose-dependent antitumor efficacy in a xenograft mice model of human colorectal cancer (HCT-116). This is approximately twice as efficacious as SAHA: SB939 causing a tumor growth inhibition of 94% versus 48% by SAHA with both at the maximum tolerated dose. Oral administration of SB939 at a dose of 50 mg/kg or 75 mg/kg in the APC^min genetic mice model of early-stage colon cancer markedly reduces the number of tumors , decreases cumulative hemocult scores and increases hematocrit values more effectively. ^[1]
動物実験	動物モデル	BALB/c nude mice bearing HCT-116 human colon cancer xenografts, Male and APC^min mice
	投与量	25, 50, 75, or 100 mg/kg
	投与経路	Oral gavage once daily

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02118909	Completed	Healthy Volunteers\|Non-smokers	Helsinn Healthcare SA	May 2014	Phase 1
NCT02058784	Completed	Healthy Volunteers\|Moderate to Heavy Smokers\|Non-smokers	Helsinn Healthcare SA\|Celerion	February 2014	Early Phase 1
NCT01112384	Completed	Metastatic Sarcoma	NCIC Clinical Trials Group\|S*BIO\|Canadian Cancer Trials Group	October 21 2010	Phase 2
NCT00741234	Completed	Solid Tumors\|Hematologic Malignancies\|Myelodysplastic Syndrome	S*BIO	April 2007	Phase 1

参考
[1] Novotny-Diermayr V, et al. Mol Cancer Ther, 2010, 9(3), 642-652.

参考

[1] Novotny-Diermayr V, et al. Mol Cancer Ther, 2010, 9(3), 642-652.

化学情報

分子量	358.48	化学式	C₂₀H₃₀N₄O₂
CAS No.	929016-96-6	SDF	Download Pracinostat (SB939) SDFをダウンロードする
Smiles	CCCCC1=NC2=C(N1CCN(CC)CC)C=CC(=C2)C=CC(=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 : 72 mg/mL ( (200.84 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 : 27 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

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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