Quisinostat(Synonyms: JNJ-26481585)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Quisinostat (Synonyms: JNJ-26481585) 纯度: 98.02%

Quisinostat (JNJ-26481585) 是一种高效的，第二代，具有口服活性的 pan-HDAC 抑制剂 (HDACi)，对 HDAC1、HDAC2、HDAC4、HDAC10、HDAC11 作用的 IC50 值范围为 0.11-0.64 nM。Quisinostat 具有广泛的抗肿瘤活性。Quisinostat 在成神经细胞瘤中能诱导自噬 (autophagy)

Quisinostat(Synonyms: JNJ-26481585)

Quisinostat Chemical Structure

CAS No. : 875320-29-9

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10 mM * 1 mL in DMSO ￥1650 In-stock
2 mg ￥900 In-stock
5 mg ￥1500 In-stock
10 mg ￥2400 In-stock
50 mg ￥7200 In-stock
100 mg ￥12000 In-stock
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Quisinostat 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Drug Repurposing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity[1]. Quisinostat can induce autophagy in neuroblastoma cells[2].

IC50 & Target[1]

HDAC1

0.11 nM (IC50)

HDAC2

0.33 nM (IC50)

HDAC4

0.64 nM (IC50)

HDAC10

0.46 nM (IC50)

HDAC11

0.37 nM (IC50)

HDAC3

4.86 nM (IC50)

HDAC5

3.69 nM (IC50)

HDAC8

4.26 nM (IC50)

HDAC9

32.1 nM (IC50)

HDAC6

76.8 nM (IC50)

HDAC7

119 nM (IC50)

体外研究
(In Vitro)

Quisinostat inhibits HDAC isozymes in vitro[1].
Quisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1].
Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[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.

Western Blot Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 24 hours
Result: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.

体内研究
(In Vivo)

Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo[1].
Quisinostat induces continuous H3 acetylation in tumor tissue in vivo[1].
Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[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.

Animal Model: NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, once daily, for 14 days
Result: Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

Clinical Trial

分子量

394.47

Formula

C21H26N6O2
CAS 号

875320-29-9
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 : 50 mg/mL (126.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5350 mL 12.6752 mL 25.3505 mL
5 mM 0.5070 mL 2.5350 mL 5.0701 mL
10 mM 0.2535 mL 1.2675 mL 2.5350 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 (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 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 (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 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 (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 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]. Arts J, et al. JNJ-26481585, a novel “second-generation” oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.

    [2]. Vamsi Krishna Kommalapati, et al. Inhibition of JNJ-26481585-mediated autophagy induces apoptosis via ROS activation and mitochondrial membrane potential disruption in neuroblastoma cells. Mol Cell Biochem. 2020 May;468(1-2):21-34.

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