Vorinostat (SAHA, MK0683)

目录号: GC17390纯度: >99.00%同义词: 伏立诺他; SAHA; Suberoylanilide hydroxamic acid

An HDAC inhibitor


Vorinostat (SAHA, MK0683)
Cas No.: 149647-78-9
规格价格库存数量操作
100mg¥200.00现货
1
500mg¥588.00现货
1
10mM (in 1mL DMSO)¥420.00现货
1

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产品描述 Description

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is a histone deacetylase inhibitor (HDACi), that plays key roles in epigenetic or non-epigenetic regulation, inducing growth arrest, differentiation and apoptosis of tumor cells.[1] Vorinostat is a small molecular with the formular of C14H20N2O3 and molecular weight of 264.3. The major mechanism of HDACi-induced apoptosis is the activation of the intrinsic apoptotic pathway. HDACi can activate the intrinsic apoptotic pathway by releasing of cytochrome c from mitochondria and regulating of Bcl-2 family expression.[2]
Vorinostat(又称亚硝基苯酰氢氧酰胺)是一种组蛋白去乙酰化酶抑制剂(HDACi),在表观遗传或非表观遗传调控中发挥重要作用,可诱导肿瘤细胞生长停滞、分化和凋亡[1]。 Vorinostat是一种小分子,化学式为C14H20N2O3,分子量为264.3。 HDACi诱导凋亡的主要机制是激活内在凋亡通路。 HDACi可以通过释放线粒体中的细胞色素c和调节Bcl-2家族表达来激活内在凋亡通路[2]。

Reference

[1] Hui-ming Z, Qian-hai D, Wei-ping C, Ru-bin L. Vorinostat, a HDAC inhibitor, showed anti-osteoarthritic activities through inhibition of iNOS and MMP expression, p38 and ERK phosphorylation and blocking NF-kB nuclear translocation. International Immunopharmacology. 2013, 17. 329-335.

[2] Norihisa U, Sayaka K, Hisanori M, Katsuhiko Y, Airo T. Requirement of p38 MAPK for a cell-death pathway triggered by vorinostat in MDA-MB-231 human breast cancer cells. Cancer Letters. 2012, 315. 112-121.

实验参考方法 Experimental Reference Method

Cell experiment: [1]

Cell lines

Human cutaneous T-cell lymphomas (CTCL) cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

IC50: 0.146 μM HH 2.062 μM HuT78 2.697 μM MJ 1.375 μM MylA 1.510 μM SeAx 72h

Applications

Vorinostat dose-dependently reduced cell proliferation with IC50 values of 0.146 μM, 2.062 μM, 2.697 μM, 1.375 μM and 1.510 μM in HH, HuT78, MJ, MylA and SeAx cells, respectively.

Animal experiment : [2]

Animal models

C57BL/6 mice bearing Eμ-myc lymphomas

Dosage form

C57BL/6 mice bearing Eμ-myc lymphomas were injected with vorinostat (200 mg/kg i.p.) and lymphoma cells were harvested after the indicated time points. The percentage of tumor cells in the lymph node of C57BL/6mice bearing Eμ-myc lymphomas treated with vorinostat was determined by FACS analysis.

Applications

Vorinostat induced a marked accumulation of Eμ-myc lymphomas displaying DNA fragmentation in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wozniak M B, Villuendas R, Bischoff J R, et al. Vorinostat interferes with the signaling transduction pathway of T cell receptor and synergizes with PI3K inhibitors in cutaneous T-cell lymphoma. haematologica, 2010: haematol. 2009.013870.

[2] Lindemann R K, Newbold A, Whitecross K F, et al. Analysis of the apoptotic and therapeutic activities of histone deacetylase inhibitors by using a mouse model of B cell lymphoma. Proceedings of the National Academy of Sciences, 2007, 104(19): 8071-8076.

产品文档 Product Documents

Purity:>99.00%

相关生物学数据Related Biological Data

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化学性质Chemical Properties

CAS 号
149647-78-9
同义词
伏立诺他; SAHA; Suberoylanilide hydroxamic acid
化学名
N'-hydroxy-N-phenyloctanediamide
SMILES
C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO
分子式
C14H20N2O3
分子量
264.3 g/mol
溶解性
≥ 4.4 mg/mL in DMSO, <2.45 mg/mL in EtOH, <2.61 mg/mL in Water
保存条件
Store at -20°C
General tips
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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol