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伏立诺他 /Vorinostat {[allProObj[0].p_purity_real_show]}

货号:A234507 同义名: N-羟基-N'-苯基辛二酰胺 / SAHA;Suberoylanilide hydroxamic acid

Vorinostat (SAHA) 是一种高效、口服活性的 HDAC1HDAC2HDAC3 (I 类)、HDAC6HDAC7 (II 类) 和 HDAC11 (IV 类) 的泛抑制剂,对 HDAC1HDAC3 的 ID50 分别为 10 nM 和 20 nM。伏立诺他诱导细胞凋亡并抑制 HPV-18 DNA 扩增。

Vorinostat 化学结构 CAS号:149647-78-9
Vorinostat 化学结构
CAS号:149647-78-9
Vorinostat 3D分子结构
CAS号:149647-78-9
Vorinostat 化学结构 CAS号:149647-78-9
Vorinostat 3D分子结构 CAS号:149647-78-9
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Vorinostat 纯度/质量文件 产品仅供科研

货号:A234507 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-A, IC50: 16 nM

HD1-B, IC50: 7.5 nM

+++

HD2, IC50: 10 nM

99%+
MC1568 ++

HD1-A (Maize), IC50: 100 nM

HD1-B (Maize), IC50: 3.4 μM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

99%+
Scriptaid 99%+
Valproic acid sodium Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

99%+
Dacinostat +++

HDAC, IC50: 32 nM

98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC8, IC50: 79.8 nM

++

HDAC9, IC50: 67.2 nM

EGFR,HER2 99%+
M344 ++

HDAC, IC50: 100 nM

99%+
Splitomicin +

Sir2p, IC50: 60 μM

95%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%+
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%+
Parthenolide p53,NF-κB 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%+
Tasquinimod 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

99%+
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

98%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%+
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

99%+
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

++++

HDAC10, IC50: 0.46 nM

++++

HDAC11, IC50: 0.37 nM

++++

HDAC2, IC50: 0.33 nM

++++

HDAC3, IC50: 4.86 nM

++++

HDAC4, IC50: 0.64 nM

++++

HDAC5, IC50: 3.69 nM

++++

HDAC8, IC50: 4.26 nM

99+%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99%+
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

99%+
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++

HDAC2, IC50: 96 nM

+++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC8, IC50: 140 nM

++

HDAC9, IC50: 70 nM

99%+
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
Lys05 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Vorinostat 生物活性

靶点
  • HDAC

    HDAC, IC50:~10 nM

描述 HDACs (Histone deacetylases) are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC 11)[1]. Vorinostat, also called as SAHA or MK0683, is a hydroxamic acid based class I and II HDACs pan inhibitor with IC50 value of 10nM on HDAC1 and 20 nM on HDAC3 (measured by immunoprecipitation–HDAC assays)[2]. Treatement with 6 μM of vorinostat in SH-SY5Y cells for 1 - 12 hours can increase the acetylation signals of histone H3 and H4 in a time-dependent manner. Vorinostat can induce cell-growth inhibition in SH-SY5Y cell line with IC50 value of 2.5 μM and 10 μM at 72h and 48h, respectively. SILAC-based quantitative MS analysis show that SAHA has a dramatic impact on histone lysine acetylation and butyrylation with strong increase in H3K9ac, H3K27ac, H2BK5bu and H4K12bu of SHSY5Y cells. Vorinostat is clinically approved for cutaneous T-cell lymphoma[3]. Both of gene expression and function of proteins regulating cell proliferation and cell death pathways are involved in the anticancer effects of SAHA, including TFIIB, Rb, Hsp90, Bcl-2 family, tubulin, HIF-1a, ROS, etc.[4].
作用机制 Vorinostat, structurally similar to TSA, chelates the zinc ion of HDACs by its hydroxamic group[5].

Vorinostat 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
22RV1 Growth Inhibition Assay IC50=2.59274 μM SANGER
5637 Growth Inhibition Assay IC50=2.32129 μM SANGER
639-V Growth Inhibition Assay IC50=3.46057 μM SANGER
647-V Growth Inhibition Assay IC50=5.99148 μM SANGER

Vorinostat 动物研究

Dose Mice (i.p.): min = 50 mg/kg[6], max = 200 mg/kg[7]
Administration i.p.
Pharmacokinetics
Animal Mice[8]
Dose 30 mg/kg
Administration i.p.
Cmax 26207 ng/ml
T1/2 0.95 h
CL/F 98 ml/min/kg
AUC0→t 5109 ng·h/ml
Vz/F 8 l/kg

Vorinostat 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00771472 Lymphoma Phase 1 Completed - -
NCT00771472 - Completed - -
NCT01064921 Stage III Squamous Cell Carcin... 展开 >>oma of the Oropharynx Stage IV Squamous Cell Carcinoma of the Oropharynx 收起 << Phase 1 Completed - United States, Ohio ... 展开 >> The Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 收起 <<

Vorinostat 参考文献

[1]Yoon S, Eom GH, et al. HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases. Chonnam Med J. 2016 Jan;52(1):1-11.

[2]Richon VM, Emiliani S, et al. A class of hybrid polar inducers of transformed cell differentiation inhibits histone deacetylases. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):3003-7.

[3]Xu G, Wang J, et al. SAHA regulates histone acetylation, Butyrylation, and protein expression in neuroblastoma. J Proteome Res. 2014 Oct 3;13(10):4211-9.

[4]Marks PA, et al. Discovery and development of SAHA as an anticancer agent. Oncogene. 2007 Feb 26;26(9):1351-6.

[5]Finnin MS, Donigian JR, et al. Structures of a histone deacetylase homologue bound to the TSA and SAHA inhibitors. Nature. 1999 Sep 9;401(6749):188-93.

[6]Hrzenjak A, Moinfar F, et al. Histone deacetylase inhibitor vorinostat suppresses the growth of uterine sarcomas in vitro and in vivo. Mol Cancer. 2010 Mar 4;9:49.

[7]Akada H, Akada S, et al. Efficacy of vorinostat in a murine model of polycythemia vera. Blood. 2012 Apr 19;119(16):3779-89.

[8]Nidhyanandan S, Thippeswamy BS, et al. Enhanced anticancer efficacy of histone deacetyl inhibitor, suberoylanilide hydroxamic acid, in combination with a phosphodiesterase inhibitor, pentoxifylline, in human cancer cell lines and in-vivo tumor xenografts. Anticancer Drugs. 2017 Oct;28(9):1002-1017.

Vorinostat 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.78mL

0.76mL

0.38mL

18.92mL

3.78mL

1.89mL

37.83mL

7.57mL

3.78mL

Vorinostat 技术信息

CAS号149647-78-9
分子式C14H20N2O3
分子量 264.32
别名 N-羟基-N'-苯基辛二酰胺 ;SAHA;Suberoylanilide hydroxamic acid;MK-0683, MK 0683, MK0683, SAHA, M344, CCRIS 8456, HSDB 7930, Vorinostat, suberoylanilide hydroxamic acid, Zolinza;MK0683
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(397.25 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+35% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

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