Dacinostat (LAQ824)

別名：NVP-LAQ824

製品コード：S1095 純度：99.17%

Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.

CAS No. 404951-53-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 63000	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 448500	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

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製品安全説明書

現在のバッチを見る：純度： 99.17%

99.17

Dacinostat (LAQ824)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
HeLa cells	Function assay	0.3 μM	16 h	Inhibition of HDAC4-mediated repression of MEF2-dependent transcription in HeLa cells at 0.3 uM after 16 hrs by luciferase reporter gene assay	17956988
H460 cells	Growth inhibition assay		48 h	Growth inhibition of human H460 cells after 48 hrs by SRB assay, IC50=0.07 μM	21073160
HCT116 cells	Growth inhibition assay		48 h	Growth inhibition of human HCT116 cells after 48 hrs by SRB assay, IC50=0.018 μM	21073160
H1299	Growth inhibition assay			Inhibitory activity against H1299 human lung carcinoma cell growth, IC50=0.15 μM	14521422
HCT116	Growth inhibition assay			Inhibitory activity against HCT116 human colon cell growth, IC50=0.01 μM	14521422
HCT116	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by MTT assay, IC50=0.05 μM	17941625
human mammary epithelial cells	Cytotoxicity assay			Cytotoxicity against human mammary epithelial cells by MTT assay, IC50=1 μM	17941625
HEK293 cells	Function assay			Inhibition of HDAC1 in HEK293 cells, IC50=0.0026 μM	18308563
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells by MTS assay, IC50=0.013 μM	20205394
H1299 cells	Proliferation assay			Antiproliferative activity against human H1299 cells by MTS assay, IC50=0.161 μM	20205394
CCRF-CEM cells	Proliferation assay			Antiproliferative activity against human CCRF-CEM cells by SRB assay, GI50=0.251 μM	21621883
K562 cells	Proliferation assay			Antiproliferative activity against human K562 cells by SRB assay, GI50=0.55 μM	21621883
MOLT4 cells	Proliferation assay			Antiproliferative activity against human MOLT4 cells by SRB assay, GI50=0.311 μM	21621883
SR cells	Proliferation assay			Antiproliferative activity against human SR cells by SRB assay, GI50=2.99 μM	21621883
A549 cells	Proliferation assay			Antiproliferative activity against human A549 cells by SRB assay, GI50=1.09 μM	21621883
EKVX cells	Proliferation assay			Antiproliferative activity against human EKVX cells by SRB assay, GI50=1.75 μM	21621883
HOP62 cells	Proliferation assay			Antiproliferative activity against human HOP62 cells by SRB assay, GI50=0.502 μM	21621883
HOP92 cells	Proliferation assay			Antiproliferative activity against human HOP92 cells by SRB assay, GI50=0.199 μM	21621883
NCI-H226 cells	Proliferation assay			Antiproliferative activity against human NCI-H226 cells by SRB assay, GI50=1.41 μM	21621883
NCI-H23 cells	Proliferation assay			Antiproliferative activity against human NCI-H23 cells by SRB assay, GI50=1.5 μM	21621883
NCI-H322M cells	Proliferation assay			Antiproliferative activity against human NCI-H322M cells by SRB assay, GI50=2.26 μM	21621883
NCI-H460 cells	Proliferation assay			Antiproliferative activity against human NCI-H460 cells by SRB assay, GI50=0.7 μM	21621883
COLO205 cells	Proliferation assay			Antiproliferative activity against human COLO205 cells by SRB assay, GI50=1.08 μM	21621883
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells by SRB assay, GI50=0.347 μM	21621883
HCT15 cells	Proliferation assay			Antiproliferative activity against human HCT15 cells by SRB assay, GI50=2.07 μM	21621883
HT-29 cells	Proliferation assay			Antiproliferative activity against human HT-29 cells by SRB assay, GI50=0.566 μM	21621883
KM12 cells	Proliferation assay			Antiproliferative activity against human KM12 cells by SRB assay, GI50=1.04 μM	21621883
SW620 cells	Proliferation assay			Antiproliferative activity against human SW620 cells by SRB assay, GI50=0.478 μM	21621883
SF268 cells	Proliferation assay			Antiproliferative activity against human SF268 cells by SRB assay, GI50=1.53 μM	21621883
SF295 cells	Proliferation assay			Antiproliferative activity against human SF295 cells by SRB assay, GI50=0.743 μM	21621883
SF539 cells	Proliferation assay			Antiproliferative activity against human SF539 cells by SRB assay, GI50=0.965 μM	21621883
SNB19 cells	Proliferation assay			Antiproliferative activity against human SNB19 cells by SRB assay, GI50=1.53 μM	21621883
SNB75 cells	Proliferation assay			Antiproliferative activity against human SNB75 cells by SRB assay, GI50=0.318 μM	21621883
U251 cells	Proliferation assay			Antiproliferative activity against human U251 cells by SRB assay, GI50=0.773 μM	21621883
LOXIMVI cells	Proliferation assay			Antiproliferative activity against human LOXIMVI cells by SRB assay, GI50=1.08 μM	21621883
MALME-3M cells	Proliferation assay			Antiproliferative activity against human MALME-3M cells by SRB assay, GI50=0.461 μM	21621883
M14 cells	Proliferation assay			Antiproliferative activity against human M14 cells by SRB assay, GI50=0.849 μM	21621883
MDA-MB-435 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-435 cells by SRB assay, GI50=0.537 μM	21621883
SK-MEL-28 cells	Proliferation assay			Antiproliferative activity against human SK-MEL-28 cells by SRB assay, GI50=0.993 μM	21621883
SK-MEL-5 cells	Proliferation assay			Antiproliferative activity against human SK-MEL-5 cells by SRB assay, GI50=0.271 μM	21621883
UACC257 cells	Proliferation assay			Antiproliferative activity against human UACC257 cells by SRB assay, GI50=0.393 μM	21621883
UACC62 cells	Proliferation assay			Antiproliferative activity against human UACC62 cells by SRB assay, GI50=0.379 μM	21621883
IGROV1 cells	Proliferation assay			Antiproliferative activity against human IGROV1 cells by SRB assay, GI50=0.187 μM	21621883
OVCAR3 cells	Proliferation assay			Antiproliferative activity against human OVCAR3 cells by SRB assay, GI50=1.11 μM	21621883
OVCAR4 cells	Proliferation assay			Antiproliferative activity against human OVCAR4 cells by SRB assay, GI50=3.21 μM	21621883
OVCAR5 cells	Proliferation assay			Antiproliferative activity against human OVCAR5 cells by SRB assay, GI50=0.26 μM	21621883
OVCAR8 cells	Proliferation assay			Antiproliferative activity against human OVCAR8 cells by SRB assay, GI50=0.45 μM	21621883
NCI/ADR-RES cells	Proliferation assay			Antiproliferative activity against human NCI/ADR-RES cells by SRB assay, GI50=0.18 μM	21621883
SKOV3 cells	Proliferation assay			Antiproliferative activity against human SKOV3 cells by SRB assay, GI50=0.524 μM	21621883
786-0 cells	Proliferation assay			Antiproliferative activity against human 786-0 cells by SRB assay, GI50=2.38 μM	21621883
A498 cells	Proliferation assay			Antiproliferative activity against human A498 cells by SRB assay, GI50=1.11 μM	21621883
ACHN cells	Proliferation assay			Antiproliferative activity against human ACHN cells by SRB assay, GI50=1.1 μM	21621883
Caki1 cells	Proliferation assay			Antiproliferative activity against human Caki1 cells by SRB assay, GI50=0.619 μM	21621883
SN12C cells	Proliferation assay			Antiproliferative activity against human SN12C cells by SRB assay, GI50=3.92 μM	21621883
TK10 cells	Proliferation assay			Antiproliferative activity against human TK10 cells by SRB assay, GI50=0.444 μM	21621883
UO31 cells	Proliferation assay			Antiproliferative activity against human UO31 cells by SRB assay, GI50=0.452 μM	21621883
PC3 cells	Proliferation assay			Antiproliferative activity against human PC3 cells by SRB assay, GI50=20 μM	21621883
DU145 cells	Proliferation assay			Antiproliferative activity against human DU145 cells by SRB assay, GI50=29.9 μM	21621883
MCF7 cells	Proliferation assay			Antiproliferative activity against human MCF7 cells by SRB assay, GI50=6.91 μM	21621883
MDA-MB-231 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-231 cells by SRB assay, GI50=31.7 μM	21621883
Hs 578T cells	Proliferation assay			Antiproliferative activity against human Hs 578T cells by SRB assay, GI50=5.82 μM	21621883
BT549 cells	Proliferation assay			Antiproliferative activity against human BT549 cells by SRB assay, GI50=6.04 μM	21621883
T47D cells	Proliferation assay			Antiproliferative activity against human T47D cells by SRB assay, GI50=28.8 μM	21621883
MDA-MB-468 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-468 cells by SRB assay, GI50=5.88 μM	21621883
NCI-H226 cells	Cytotoxicity assay			Cytotoxicity against human NCI-H226 cells, LC50=20 μM	21621883
KM12 cells	Cytotoxicity assay			Cytotoxicity against human KM12 cells, LC50=29.9 μM	21621883
SF295 cells	Cytotoxicity assay			Cytotoxicity against human SF295 cells, LC50=6.91 μM	21621883
SNB19 cells	Cytotoxicity assay			Cytotoxicity against human SNB19 cells, LC50=31.7 μM	21621883
U251 cells	Cytotoxicity assay			Cytotoxicity against human U251 cells, LC50=5.82 μM	21621883
LOXIMVI cells	Cytotoxicity assay			Cytotoxicity against human LOXIMVI cells, LC50=6.04 μM	21621883
MDA-MB-435 cells	Cytotoxicity assay			Cytotoxicity against human MDA-MB-435 cells, LC50=28.8 μM	21621883
SK-MEL-28 cells	Cytotoxicity assay			Cytotoxicity against human SK-MEL-28 cells, LC50=31.9 μM	21621883
SK-MEL-5 cells	Cytotoxicity assay			Cytotoxicity against human SK-MEL-5 cells, LC50=4.02 μM	21621883
UACC257 cells	Cytotoxicity assay			Cytotoxicity against human UACC257 cells, LC50=44.8 μM	21621883
UACC62 cells	Cytotoxicity assay			Cytotoxicity against human UACC62 cells, LC50=6.39 μM	21621883
IGROV1 cells	Cytotoxicity assay			Cytotoxicity against human IGROV1 cells, LC50=48.9 μM	21621883
OVCAR5 cells	Cytotoxicity assay			Cytotoxicity against human OVCAR5 cells, LC50=38.9 μM	21621883
SKOV3 cells	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells, LC50=28.5 μM	21621883
A498 cells	Cytotoxicity assay			Cytotoxicity against human A498 cells, LC50=5.88 μM	21621883
Caki1 cells	Cytotoxicity assay			Cytotoxicity against human Caki1 cells, LC50=5.79 μM	21621883
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells, IC50=0.019 μM	21742496
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50=0.019 μM	21650221
H1299 cells	Proliferation assay			Antiproliferative activity against human H1299 cells, IC50=0.1 μM	21650221
HCT116 cells	Proliferation assay			Inhibitory concentration against HCT116 cells proliferation, IC50=0.01 μM	14613312
RPMI8226 cells	Proliferation assay			Antiproliferative activity against human RPMI8226 cells by SRB assay, GI50=0.523 μM	21621883
CHO cells	Function assay			Inhibition of human ERG expressed in CHO cells by automated patch clamp electrophysiology assay, IC50=12.2 μM	20205394
HL-60(TB) cells	Proliferation assay			Antiproliferative activity against human HL-60(TB) cells by SRB assay, GI50=0.249 μM	21621883
RXF393 cells	Proliferation assay			Antiproliferative activity against human RXF393 cells by SRB assay, GI50=0.01 μM	21621883
RXF393 cells	Cytotoxicity assay			Cytotoxicity against human RXF393 cells, LC50=15.3 μM	21621883
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Dacinostat (LAQ824, NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.

Targets

p21 ^[1]	HDAC ^[1] (Cell-free assay)
	32 nM

In Vitro
In vitro	LAQ824 activates the expression of the gene encoding the p21 cell cycle inhibitor by activating the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM. LAQ824 inhibits the cell growth of both H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively, and the antiproliferative effect of LAQ824 is selective toward the tumor cell lines while inducing only growth arrest in normal fibroblasts. Furthermore, LAQ824 induces a dose-dependent increase of p21 protein in A549 cells and an increase in the hypophosphorylated state of the Rb tumor suppressor. ^[1] A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages. ^[2]
Kinase Assay	In Vitro Histone Deacetylase Assay
Kinase Assay	HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl₂, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO₄, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-³²P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.
細胞実験	細胞株	H1299, HCT116, DU145, PC3 and MDA435 cells
	濃度	0-10 μM
	反応時間	48 hours
	実験の流れ	Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If X0, %Growth=(X-T₀)/T₀100; If X>T₀, %Growth=(X-T₀)/(GC-T₀)100. where T₀ is the average value of T₀ − background, GC is the average value of untreated cells (in triplicate) − background, and X is the average value of compound-treated cells (in triplicate)-background. The “% Growth” is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.

In Vivo
In Vivo	In HCT116 and human colon tumor xenografts in nude mice, LAQ824 treatment at 100 mg/kg produces the inhibitory effects on tumor growth in a dose-dependent mode without general cytotoxicity. ^[1]
動物実験	動物モデル	HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
	投与量	≤100 mg/kg
	投与経路	Administered via i.v.

参考
[1] Atadja P, et al. Cancer Res, 2004, 64(2), 689-695. [2] Wang H, et al. J Immuno, 2011, 186(7), 3986-3996.

参考

化学情報

分子量	379.459	化学式	C₂₂H₂₅N₃O₃
CAS No.	404951-53-7	SDF	Download Dacinostat (LAQ824) SDFをダウンロードする
Smiles	C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=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 : 76 mg/mL ( (200.28 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

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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
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):