Dacinostat (LAQ824)
别名: NVP-LAQ824 中文名称：达诺司他
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
产品质控
批次：
纯度：
99.17%
99.17
Dacinostat (LAQ824)相关产品
相关信号通路图
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 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 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 |
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| 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 | |||
| 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 | |
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) | |||
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体外溶解度 |
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 |
|
体内溶解度 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 | ||||
实验计算
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）
mg/kg
g
μL
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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