Dacinostat(Synonyms: NVP-LAQ824; LAQ824)

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Dacinostat (Synonyms: NVP-LAQ824; LAQ824) 纯度: 98.45%

Dacinostat 是一种有效的 HDAC 抑制剂,IC50 值为 32 nM;Dacinostat 同时可抑制 HDAC1 的活性,IC50 值为 9 nM,主要用于癌症研究。

Dacinostat(Synonyms: NVP-LAQ824;  LAQ824)

Dacinostat Chemical Structure

CAS No. : 404951-53-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥2380 In-stock
10 mg ¥2160 In-stock
50 mg ¥5760 In-stock
100 mg   询价  
200 mg   询价  

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Dacinostat 相关产品

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生物活性

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

IC50 & Target

HDAC1

9 nM (IC50)

HDAC

32 nM (IC50)

体外研究
(In Vitro)

Dacinostat (NVP-LAQ824) activates p21 promoter, with AC50 of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC50s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC50s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4[1]. Dacinostat inhibits HDAC1 with an IC50 of 9 nM[2]. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

379.45

Formula

C22H25N3O3

CAS 号

404951-53-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 43 mg/mL (113.32 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.59 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Atadja P, et al. Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824. Cancer Res. 2004 Jan 15;64(2):689-95.

    [2]. Cho YS, et al. Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824). J Med Chem. 2010 Apr 8;53(7):2952-63.

    [3]. Romanski A, et al. Deacetylase inhibitors modulate proliferation and self-renewal properties of leukemic stem and progenitor cells. Cell Cycle. 2012 Sep 1;11(17):3219-26.

Kinase Assay
[2]

The HDAC enzymatic assay measures compound activity in inhibiting purified HDAC isoforms. HDACs 1, 3, and 6 are immunopurified from 293 cells stably expressing the FLAG-tagged HDAC isoform, whereas HDACs 2, 4, 5, 7, 8, 9, 10, and 11 are purified from the baculovirus expression system. HDAC activity is measured in a fluorescent assay in which deacetylation of the substrate, bis-Boc-(Ac)Lys-rhodamine 110, generates a fluorophore that can be detected on a fluorometric plate reader[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cells are plated at 5000−10000 cells per well in 96-well plates and treated with eight serial compound dilutions. Cell viability following 72 h of compound treatment is measured using the CellTiter-Glo or MTS assay. XLfit 4 is used for plotting of the growth curves and calculation of IC50 values[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

The studies are performed on-site, using outbred athymic (nu/nu) female mice. Mice are anesthetized with Metofane, and a cell suspension (100 μL) containing 1×106 HCT116 cells is injected s.c. into the right axillary (lateral) region of each animal. Tumors are allowed to reach the volume of approximately 100-400 mm3. At this point, mice bearing tumors with acceptable morphology (non-necrotic) and of similar size range are selected and distributed into groups of six for the studies. NVP-LAQ824 is dissolved in DMSO to create a stock solution, which is further diluted just before dosing with D5W to a final DMSO concentration of 10%. Tumor-bearing mice are treated with the compound by i.v. injection into the tail vein. NVP-LAQ824 is dosed once daily, 5 days/week, for a total of 15 doses. 5-Fluorouracil is administered at 100 mg/kg in 0.9% saline 1 day/week for a total of three doses. The control groups are treated with the vehicle. Tumors are collected from the animals at the indicated time points[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Atadja P, et al. Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824. Cancer Res. 2004 Jan 15;64(2):689-95.

    [2]. Cho YS, et al. Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824). J Med Chem. 2010 Apr 8;53(7):2952-63.

    [3]. Romanski A, et al. Deacetylase inhibitors modulate proliferation and self-renewal properties of leukemic stem and progenitor cells. Cell Cycle. 2012 Sep 1;11(17):3219-26.

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