Dacinostat (LAQ824)

別名: NVP-LAQ824 中文名稱：達諾司他

目錄號：S1095 Purity: 99.17%

Dacinostat (LAQ824, NVP-LAQ824)是新型HDAC抑制劑，IC50為32 nM，且激活p21啟動子。

Dacinostat (LAQ824) Chemical Structure

CAS: 404951-53-7

規(guī)格	價格	庫存
10mM (1mL in DMSO)	3444.22	現(xiàn)貨
10mg	2609.75	現(xiàn)貨
50mg	7958.15	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.17%

99.17

Dacinostat (LAQ824)相關(guān)產(chǎn)品

相關(guān)靶點	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	點擊展開
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相關(guān)化合物庫	激酶抑制劑庫 FDA藥物庫天然產(chǎn)物庫已知活性藥物庫-I 高選擇性抑制劑庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述
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
H460 cells	Growth inhibition assay		48 h	Growth inhibition of human H460 cells after 48 hrs by SRB assay, IC50=0.07 μM
HCT116 cells	Growth inhibition assay		48 h	Growth inhibition of human HCT116 cells after 48 hrs by SRB assay, IC50=0.018 μM
H1299	Growth inhibition assay			Inhibitory activity against H1299 human lung carcinoma cell growth, IC50=0.15 μM
HCT116	Growth inhibition assay			Inhibitory activity against HCT116 human colon cell growth, IC50=0.01 μM
HCT116	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by MTT assay, IC50=0.05 μM
human mammary epithelial cells	Cytotoxicity assay			Cytotoxicity against human mammary epithelial cells by MTT assay, IC50=1 μM
HEK293 cells	Function assay			Inhibition of HDAC1 in HEK293 cells, IC50=0.0026 μM
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells by MTS assay, IC50=0.013 μM
H1299 cells	Proliferation assay			Antiproliferative activity against human H1299 cells by MTS assay, IC50=0.161 μM
CCRF-CEM cells	Proliferation assay			Antiproliferative activity against human CCRF-CEM cells by SRB assay, GI50=0.251 μM
K562 cells	Proliferation assay			Antiproliferative activity against human K562 cells by SRB assay, GI50=0.55 μM
MOLT4 cells	Proliferation assay			Antiproliferative activity against human MOLT4 cells by SRB assay, GI50=0.311 μM
SR cells	Proliferation assay			Antiproliferative activity against human SR cells by SRB assay, GI50=2.99 μM
A549 cells	Proliferation assay			Antiproliferative activity against human A549 cells by SRB assay, GI50=1.09 μM
EKVX cells	Proliferation assay			Antiproliferative activity against human EKVX cells by SRB assay, GI50=1.75 μM
HOP62 cells	Proliferation assay			Antiproliferative activity against human HOP62 cells by SRB assay, GI50=0.502 μM
HOP92 cells	Proliferation assay			Antiproliferative activity against human HOP92 cells by SRB assay, GI50=0.199 μM
NCI-H226 cells	Proliferation assay			Antiproliferative activity against human NCI-H226 cells by SRB assay, GI50=1.41 μM
NCI-H23 cells	Proliferation assay			Antiproliferative activity against human NCI-H23 cells by SRB assay, GI50=1.5 μM
NCI-H322M cells	Proliferation assay			Antiproliferative activity against human NCI-H322M cells by SRB assay, GI50=2.26 μM
NCI-H460 cells	Proliferation assay			Antiproliferative activity against human NCI-H460 cells by SRB assay, GI50=0.7 μM
COLO205 cells	Proliferation assay			Antiproliferative activity against human COLO205 cells by SRB assay, GI50=1.08 μM
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells by SRB assay, GI50=0.347 μM
HCT15 cells	Proliferation assay			Antiproliferative activity against human HCT15 cells by SRB assay, GI50=2.07 μM
HT-29 cells	Proliferation assay			Antiproliferative activity against human HT-29 cells by SRB assay, GI50=0.566 μM
KM12 cells	Proliferation assay			Antiproliferative activity against human KM12 cells by SRB assay, GI50=1.04 μM
SW620 cells	Proliferation assay			Antiproliferative activity against human SW620 cells by SRB assay, GI50=0.478 μM
SF268 cells	Proliferation assay			Antiproliferative activity against human SF268 cells by SRB assay, GI50=1.53 μM
SF295 cells	Proliferation assay			Antiproliferative activity against human SF295 cells by SRB assay, GI50=0.743 μM
SF539 cells	Proliferation assay			Antiproliferative activity against human SF539 cells by SRB assay, GI50=0.965 μM
SNB19 cells	Proliferation assay			Antiproliferative activity against human SNB19 cells by SRB assay, GI50=1.53 μM
SNB75 cells	Proliferation assay			Antiproliferative activity against human SNB75 cells by SRB assay, GI50=0.318 μM
U251 cells	Proliferation assay			Antiproliferative activity against human U251 cells by SRB assay, GI50=0.773 μM
LOXIMVI cells	Proliferation assay			Antiproliferative activity against human LOXIMVI cells by SRB assay, GI50=1.08 μM
MALME-3M cells	Proliferation assay			Antiproliferative activity against human MALME-3M cells by SRB assay, GI50=0.461 μM
M14 cells	Proliferation assay			Antiproliferative activity against human M14 cells by SRB assay, GI50=0.849 μM
MDA-MB-435 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-435 cells by SRB assay, GI50=0.537 μM
SK-MEL-28 cells	Proliferation assay			Antiproliferative activity against human SK-MEL-28 cells by SRB assay, GI50=0.993 μM
SK-MEL-5 cells	Proliferation assay			Antiproliferative activity against human SK-MEL-5 cells by SRB assay, GI50=0.271 μM
UACC257 cells	Proliferation assay			Antiproliferative activity against human UACC257 cells by SRB assay, GI50=0.393 μM
UACC62 cells	Proliferation assay			Antiproliferative activity against human UACC62 cells by SRB assay, GI50=0.379 μM
IGROV1 cells	Proliferation assay			Antiproliferative activity against human IGROV1 cells by SRB assay, GI50=0.187 μM
OVCAR3 cells	Proliferation assay			Antiproliferative activity against human OVCAR3 cells by SRB assay, GI50=1.11 μM
OVCAR4 cells	Proliferation assay			Antiproliferative activity against human OVCAR4 cells by SRB assay, GI50=3.21 μM
OVCAR5 cells	Proliferation assay			Antiproliferative activity against human OVCAR5 cells by SRB assay, GI50=0.26 μM
OVCAR8 cells	Proliferation assay			Antiproliferative activity against human OVCAR8 cells by SRB assay, GI50=0.45 μM
NCI/ADR-RES cells	Proliferation assay			Antiproliferative activity against human NCI/ADR-RES cells by SRB assay, GI50=0.18 μM
SKOV3 cells	Proliferation assay			Antiproliferative activity against human SKOV3 cells by SRB assay, GI50=0.524 μM
786-0 cells	Proliferation assay			Antiproliferative activity against human 786-0 cells by SRB assay, GI50=2.38 μM
A498 cells	Proliferation assay			Antiproliferative activity against human A498 cells by SRB assay, GI50=1.11 μM
ACHN cells	Proliferation assay			Antiproliferative activity against human ACHN cells by SRB assay, GI50=1.1 μM
Caki1 cells	Proliferation assay			Antiproliferative activity against human Caki1 cells by SRB assay, GI50=0.619 μM
SN12C cells	Proliferation assay			Antiproliferative activity against human SN12C cells by SRB assay, GI50=3.92 μM
TK10 cells	Proliferation assay			Antiproliferative activity against human TK10 cells by SRB assay, GI50=0.444 μM
UO31 cells	Proliferation assay			Antiproliferative activity against human UO31 cells by SRB assay, GI50=0.452 μM
PC3 cells	Proliferation assay			Antiproliferative activity against human PC3 cells by SRB assay, GI50=20 μM
DU145 cells	Proliferation assay			Antiproliferative activity against human DU145 cells by SRB assay, GI50=29.9 μM
MCF7 cells	Proliferation assay			Antiproliferative activity against human MCF7 cells by SRB assay, GI50=6.91 μM
MDA-MB-231 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-231 cells by SRB assay, GI50=31.7 μM
Hs 578T cells	Proliferation assay			Antiproliferative activity against human Hs 578T cells by SRB assay, GI50=5.82 μM
BT549 cells	Proliferation assay			Antiproliferative activity against human BT549 cells by SRB assay, GI50=6.04 μM
T47D cells	Proliferation assay			Antiproliferative activity against human T47D cells by SRB assay, GI50=28.8 μM
MDA-MB-468 cells	Proliferation assay			Antiproliferative activity against human MDA-MB-468 cells by SRB assay, GI50=5.88 μM
NCI-H226 cells	Cytotoxicity assay			Cytotoxicity against human NCI-H226 cells, LC50=20 μM
KM12 cells	Cytotoxicity assay			Cytotoxicity against human KM12 cells, LC50=29.9 μM
SF295 cells	Cytotoxicity assay			Cytotoxicity against human SF295 cells, LC50=6.91 μM
SNB19 cells	Cytotoxicity assay			Cytotoxicity against human SNB19 cells, LC50=31.7 μM
U251 cells	Cytotoxicity assay			Cytotoxicity against human U251 cells, LC50=5.82 μM
LOXIMVI cells	Cytotoxicity assay			Cytotoxicity against human LOXIMVI cells, LC50=6.04 μM
MDA-MB-435 cells	Cytotoxicity assay			Cytotoxicity against human MDA-MB-435 cells, LC50=28.8 μM
SK-MEL-28 cells	Cytotoxicity assay			Cytotoxicity against human SK-MEL-28 cells, LC50=31.9 μM
SK-MEL-5 cells	Cytotoxicity assay			Cytotoxicity against human SK-MEL-5 cells, LC50=4.02 μM
UACC257 cells	Cytotoxicity assay			Cytotoxicity against human UACC257 cells, LC50=44.8 μM
UACC62 cells	Cytotoxicity assay			Cytotoxicity against human UACC62 cells, LC50=6.39 μM
IGROV1 cells	Cytotoxicity assay			Cytotoxicity against human IGROV1 cells, LC50=48.9 μM
OVCAR5 cells	Cytotoxicity assay			Cytotoxicity against human OVCAR5 cells, LC50=38.9 μM
SKOV3 cells	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells, LC50=28.5 μM
A498 cells	Cytotoxicity assay			Cytotoxicity against human A498 cells, LC50=5.88 μM
Caki1 cells	Cytotoxicity assay			Cytotoxicity against human Caki1 cells, LC50=5.79 μM
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells, IC50=0.019 μM
HCT116 cells	Proliferation assay			Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50=0.019 μM
H1299 cells	Proliferation assay			Antiproliferative activity against human H1299 cells, IC50=0.1 μM
HCT116 cells	Proliferation assay			Inhibitory concentration against HCT116 cells proliferation, IC50=0.01 μM
RPMI8226 cells	Proliferation assay			Antiproliferative activity against human RPMI8226 cells by SRB assay, GI50=0.523 μM
CHO cells	Function assay			Inhibition of human ERG expressed in CHO cells by automated patch clamp electrophysiology assay, IC50=12.2 μM
HL-60(TB) cells	Proliferation assay			Antiproliferative activity against human HL-60(TB) cells by SRB assay, GI50=0.249 μM
RXF393 cells	Proliferation assay			Antiproliferative activity against human RXF393 cells by SRB assay, GI50=0.01 μM
RXF393 cells	Cytotoxicity assay			Cytotoxicity against human RXF393 cells, LC50=15.3 μM
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生物活性

產(chǎn)品描述

Dacinostat (LAQ824, NVP-LAQ824)是新型HDAC抑制劑，IC50為32 nM，且激活p21啟動子。

特性

LAQ824是非常有效的組蛋白脫乙酰基酶抑制劑。

靶點

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

體外研究(In Vitro)
體外研究活性	在體外, LAQ824抑制 H1299細胞裂解液中的人HDAC活性， IC50 為32 nM。此外, LAQ824通過激活p21 啟動子，也激活編碼p21 細胞周期抑制劑的基因表達，最大啟動子活性 (AC50)為50%時，濃度為0.30 μM。^[1] 處理72小時后, LAQ824抑制 H1299（一種非小細胞肺癌細胞）和HCT116（一種結(jié)腸癌細胞）細胞生長，IC50分別為0.15 μM和 0.01 μM, LAQ824的抗增殖效果選擇性作用于腫瘤細胞系。而且, LAQ824作用于A549細胞，促進p21蛋白增多，這種作用存在劑量依賴性，且提高Rb腫瘤抑制基因的次磷酸化狀態(tài)。^[1]最新研究顯示LAQ824在IL-10基因啟動子水平誘導(dǎo)染色體變化，導(dǎo)致轉(zhuǎn)錄抑制劑HDAC11和PU.1招募增強，且抑制BALB/c巨噬細胞中IL-10產(chǎn)量。^[2]
激酶實驗	體外組蛋白脫乙酰基酶實驗
激酶實驗	通過離子交換層析，使用Q 瓊脂糖快速流動柱，使HDAC酶部分從H1299細胞溶解物中純化。通過與cdk2多克隆抗體或cdk1/cdc2單克隆抗體進行免疫沉淀反應(yīng)，從500 mg 全部細胞溶解物中收集酶復(fù)合物。免疫沉淀物再懸浮在激酶buffer (50 mM Hepes, pH 8, 10 mM MgCl₂, 2.5 mM EDTA, 1 mM 二硫蘇糖醇, 20 mM ATP, 10 mM β-甘油磷酸, 0.1 mM NaVO₄, 1 mM NaF, 50 mM ATP, 10 μCi [γ-³²P]ATP),及1 μg pRb 重組蛋白底物(cdk2)或含 20 μg 底物(cdc2)到的10 mL H1組蛋白混合物。電泳分析磷酸化的Rb和 H1 組蛋白，然后使用PhosphorImager量化。
細胞實驗	細胞系	H1299, HCT116, DU145, PC3 和 MDA435
	濃度	0 到10 μM
	孵育時間	48小時
	方法	通過3-MTS實驗測定細胞增殖。然后進行CellTiter 96 AQueous 非放射性細胞增殖實驗。取每組實驗的平均值。

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	LAQ824按100 mg/kg 劑量作用于攜帶HCT116和人結(jié)腸癌移植瘤的裸鼠，抑制腫瘤生長，且無細胞毒性，這種作用存在劑量依賴性。^[1]
動物實驗	Animal Models	在右腋區(qū)皮下注射HCT116細胞的遠系繁殖系無胸腺(nu/nu)雌鼠
	Dosages	≤100 mg/kg
	Administration	靜脈注射

參考文獻
https://pubmed.ncbi.nlm.nih.gov/14744786/ https://pubmed.ncbi.nlm.nih.gov/21368229/

參考文獻

https://pubmed.ncbi.nlm.nih.gov/14744786/
https://pubmed.ncbi.nlm.nih.gov/21368229/

化學信息&溶解度

分子量	379.459	分子式	C₂₂H₂₅N₃O₃
CAS號	404951-53-7	SDF	Download Dacinostat (LAQ824) SDF
Smiles	C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 76 mg/mL ( (200.28 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL ( (200.28 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動物體內(nèi)配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	4% DMSO 1 40% PEG300 2 56%saline 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	3.760mg/ml (9.91mM)	以 1 mL 工作液為例,取40 μL 94mg/ml的澄清DMSO儲備液加到400 μL PEG300中,混合均勻使其澄清;然后繼續(xù)加入560 μL生理鹽水定容至1mL。工作液請現(xiàn)配現(xiàn)用!
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊

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