Panobinostat (LBH589)

別名：NVP-LBH589

製品コード：S1030 純度：99.96%

Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.

CAS No. 404950-80-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 40500	国内在庫あり
200mg	JPY 100500	国内在庫あり
1g	JPY 220500	国内在庫あり

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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現在のバッチを見る：純度： 99.96%

99.96

Panobinostat (LBH589)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
SK-N-BE	Apoptosis Assay	0–40 nM	48 h	potently induced apoptosis in a dose-dependent fashion	24098799
SK-N-SH	Apoptosis Assay	0–40 nM	48 h	potently induced apoptosis in a dose-dependent fashion	24098799
SK-N-DZ	Apoptosis Assay	0–80 nM	48 h	potently induced apoptosis in a dose-dependent fashion	24098799
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生物活性

製品説明

Targets

HDAC (MOLT-4 cells) ^[1]	HDAC (Reh cells) ^[1]
5 nM	20 nM

In Vitro
In vitro	LBH589 induces apoptosis among MOLT-4 and Reh cells in a time- and dose-dependent manner. Moreover, LBH589 is more potent in MOLT-4 than in Reh cells. LBH589 markedly prevents the growth of both MOLT-4 and Reh cells in a dose-dependent manner at 48 hours. LBH589 treatment causes a 2- to 3-fold increase in the number of cells in the G2/M phase of the cell cycle compared with the control cells. LBH589 is associated with induction of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. LBH589 treatment also increases the levels of p21 expression. LBH589 treatment also decreases the levels of c-Myc after an initial increase at the lowest dose (10 nM) in Reh cells. In addition, LBH589 gives rise to substantial increases in mRNA levels of proapoptosis and DNA repair genes. LBH589 induces increased levels of acetylated histone H3 and H4 at the GADD45G promoter. ^[1] Besides, LBH589 inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively). ^[2]
細胞実験	細胞株	MOLT-4 cell lines and Reh (pre-B cells)
	濃度	50 nM
	反応時間	48 hours
	実験の流れ	Untreated and LBH589-treated cells [human Ph- acute lymphoblastic leukemia MOLT-4 (T cells) and Reh (pre-B cells)] are stained with annexin V and propidium iodide using annexin V-FITC apoptosis detection kit I. The percentage of apoptotic and nonviable cells is determined by flow cytometry. At least 5 × 10⁴ cells are collected with a CyAn ADP Violet cytometer. Percentage apoptosis is calculated considering all the annexin V-positive plus the annexin V/PI-positive cells; percentage loss of cell viability is calculated considering all the annexin V-positive plus the PI-positive and the annexinV/PI-positive cells.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	DNMT1 / EZH2 caspase-8 / cleaved caspase-8 / Sp1 c-Myc / IRF4 Ac-H3 / cleaved caspase-3 / CCND1 / ID1 / ID2 / ID3 / ID4 / Synaptophysin / NeuroD1 RAD51 / BRCA1 / CHK1 / RPL13a H3K9AC / H3K18AC / H3K56AC / H3 / H4K8AC / H4K16AC / H4 / p21 / p27 / cleaved PARP		19279403
	Immunofluorescence	Synaptophysin / NACM α-tubulin / Acetyl-α-tubulin BiP ATF4 IRE1α / S724-IRE1α		28915627
	Growth inhibition assay	Cell viability		27738323

In Vivo
In Vivo	In lung cancer and mesothelioma animal models, LBH589 markedly decreases tumor growth by 62%. LBH589 is equally effective in immunocompetent and severe combined immunodeficien-cymice, suggesting that the inhibition of tumor growth by LBH589 is not due to direct immunologic effects. Daily LBH589, given i.p. at 20 mg/kg for 5 days per week, leading to an average decrease in growth of 70%. Compared with the corresponding control tumors, LBH589 leads to a 53% decrease for H526-derived tumors, an 81% decrease for BK-T-derived tumors, a 76% decrease for RG-1- derived tumors, and a 70% decrease for H69-derived tumors. In contrast to the lack of tumor regression notes in NSCLC and Meso-derived xenografted tumors that are treated under identical conditions and doses, LBH589 results in dramatic tumor regression in SCLC-derived tumors and RG-1-derived tumor. ^[2]
動物実験	動物モデル	Severe combined immunodeficiency (SCID) mice with M30 (10⁷ cells) or A549 (5 × 10⁶ cells), H69 (2.5 × 10⁶ cells), BK-T (6.5 × 10⁶), H526 (10 × 10⁶), and RG1 (10 × 10⁶) cells
	投与量	10 mg/kg, 20 mg/kg
	投与経路	Administered via i.p. injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04341311	Terminated	Diffuse Intrinsic Pontine Glioma\|Pediatric Brainstem Glioma\|Pediatric Brainstem Gliosarcoma Recurrent\|Pediatric Cancer\|Pediatric Brain Tumor\|Diffuse Glioma	Dana-Farber Cancer Institute\|Celgene\|Secura Bio Inc.	August 10 2020	Phase 1
NCT03632317	Withdrawn	Glioma\|Diffuse Intrinsic Pontine Glioma	University of Michigan Rogel Cancer Center	October 2019	Phase 2
NCT03982134	Withdrawn	Melanoma\|Non Small Cell Lung Cancer	Muhammad Furqan\|Novartis Pharmaceuticals\|University of Iowa	September 2019	Phase 1
NCT04326764	Terminated	Acute Myeloid Leukaemia (AML)\|Myelodysplastic Syndromes (MDS)	Goethe University\|Stichting Hemato-Oncologie voor Volwassenen Nederland\|Polish Adult Leukemia Group\|Schweizerische Arbeitsgemeinschaft für klinische Krebsforschung	July 24 2018	Phase 3
NCT03515915	Unknown status	Patients With Recurrent or Refractory Multiple Myeloma	University Hospital Montpellier\|Poitiers University Hospital	April 23 2018	--

参考
[1] Scuto A, et al. Blood. 2008, 111(10), 5093-5100. [2] Crisanti MC, et al. Mol Cancer Ther. 2009, 8(8), 2221-2231. [3] Ocio EM, et al. Haematologica, 2010, 95(5), 794-803. [4] Maiso P, et al. Cancer Res, 2006, 66(11), 5781-5789. [5] Atadja P, Cancer Lett, 2009, 280(2), 233-241. + 展開

参考

+ 展開

化学情報

分子量	349.43	化学式	C₂₁H₂₃N₃O₂
CAS No.	404950-80-7	SDF	Download Panobinostat (LBH589) SDFをダウンロードする
Smiles	CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)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 : 70 mg/mL ( (200.32 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。)

Water : Insoluble

Ethanol : 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 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O

2.5mg/ml (7.15mM)

Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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:
How to reconstitute the compound for in vivo mice study?

回答
We recommend the vehicle is 2 % DMSO, 2 % Tween 80, 48%PEG300, 48% water. The compound is first dissolved in DMSO, then add Tween, PEG300, water in sequence.

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C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):