Dacinostat (LAQ824)

别名: NVP-LAQ824 中文名称：达诺司他

目录号：S1095 Purity: 99.17%

Dacinostat (LAQ824, NVP-LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。

Dacinostat (LAQ824) Chemical Structure

CAS: 404951-53-7

规格	价格	库存
10mM (1mL in DMSO)	3444.22	现货
10mg	2609.75	现货
50mg	7958.15	现货
1g	24488.1	现货
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产品质控

批次：纯度： 99.17%

99.17

Dacinostat (LAQ824)相关产品

相关靶点	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	点击展开
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相关化合物库	激酶抑制剂库 FDA药物库天然产物库已知活性药物库-I 高选择性抑制剂库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	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
点击查看更多细胞系数据

生物活性

产品描述

Dacinostat (LAQ824, NVP-LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。

特性

LAQ824是非常有效的组蛋白脱乙酰基酶抑制剂。

靶点

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

体外研究(In Vitro)
体外研究活性	在体外, LAQ824抑制 H1299细胞裂解液中的人HDAC活性， IC50 为32 nM。此外, LAQ824通过激活p21 启动子，也激活编码p21 细胞周期抑制剂的基因表达，最大启动子活性 (AC50)为50%时，浓度为0.30 μM。^[1] 处理72小时后, LAQ824抑制 H1299（一种非小细胞肺癌细胞）和HCT116（一种结肠癌细胞）细胞生长，IC50分别为0.15 μM和 0.01 μM, LAQ824的抗增殖效果选择性作用于肿瘤细胞系。而且, LAQ824作用于A549细胞，促进p21蛋白增多，这种作用存在剂量依赖性，且提高Rb肿瘤抑制基因的次磷酸化状态。^[1]最新研究显示LAQ824在IL-10基因启动子水平诱导染色体变化，导致转录抑制剂HDAC11和PU.1招募增强，且抑制BALB/c巨噬细胞中IL-10产量。^[2]
激酶实验	体外组蛋白脱乙酰基酶实验
激酶实验	通过离子交换层析，使用Q 琼脂糖快速流动柱，使HDAC酶部分从H1299细胞溶解物中纯化。通过与cdk2多克隆抗体或cdk1/cdc2单克隆抗体进行免疫沉淀反应，从500 mg 全部细胞溶解物中收集酶复合物。免疫沉淀物再悬浮在激酶buffer (50 mM Hepes, pH 8, 10 mM MgCl₂, 2.5 mM EDTA, 1 mM 二硫苏糖醇, 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 重组蛋白底物(cdk2)或含 20 μg 底物(cdc2)到的10 mL H1组蛋白混合物。电泳分析磷酸化的Rb和 H1 组蛋白，然后使用PhosphorImager量化。
细胞实验	细胞系	H1299, HCT116, DU145, PC3 和 MDA435
	浓度	0 到10 μM
	孵育时间	48小时
	方法	通过3-MTS实验测定细胞增殖。然后进行CellTiter 96 AQueous 非放射性细胞增殖实验。取每组实验的平均值。

体内研究(In Vivo)
体内研究活性	LAQ824按100 mg/kg 剂量作用于携带HCT116和人结肠癌移植瘤的裸鼠，抑制肿瘤生长，且无细胞毒性，这种作用存在剂量依赖性。^[1]
动物实验	Animal Models	在右腋区皮下注射HCT116细胞的远系繁殖系无胸腺(nu/nu)雌鼠
	Dosages	≤100 mg/kg
	Administration	静脉注射

参考文献
https://pubmed.ncbi.nlm.nih.gov/14744786/ https://pubmed.ncbi.nlm.nih.gov/21368229/

参考文献

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

化学信息&溶解度

分子量	379.459	分子式	C₂₂H₂₅N₃O₃
CAS号	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
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 76 mg/mL ( (200.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 76 mg/mL ( (200.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	4% DMSO 1 40% PEG300 2 56%saline 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.760mg/ml (9.91mM)	以 1 mL 工作液为例,取40 μL 94mg/ml的澄清DMSO储备液加到400 μL PEG300中,混合均匀使其澄清;然后继续加入560 μL生理盐水定容至1mL。工作液请现配现用!
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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