伏立诺他

Vorinostat(SAHA)

	产品编号	CFN60012
	CAS编号	149647-78-9
	分子式 = 分子量	C₁₄H₂₀N₂O₃ = 264.3
	产品纯度	>=98%
	物理属性	Powder
	化合物类型	Alkaloids
	植物来源
ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用

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产品名称	产品编号	CAS编号	包装	QQ客服
伏立诺他	CFN60012	149647-78-9	1mg	QQ客服：3257982914
伏立诺他	CFN60012	149647-78-9	5mg	QQ客服：3257982914
伏立诺他	CFN60012	149647-78-9	10mg	QQ客服：3257982914
伏立诺他	CFN60012	149647-78-9	20mg	QQ客服：3257982914

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ChemFaces的产品在许多优秀和顶级科学期刊中被引用

Cell. 2018 Jan 11;172(1-2):249-261.e12.
doi: 10.1016/j.cell.2017.12.019.
IF=36.216(2019)

PMID: 29328914

Cell Metab. 2020 Mar 3;31(3):534-548.e5.
doi: 10.1016/j.cmet.2020.01.002.
IF=22.415(2019)

PMID: 32004475

Mol Cell. 2017 Nov 16;68(4):673-685.e6.
doi: 10.1016/j.molcel.2017.10.022.
IF=14.548(2019)

PMID: 29149595

ACS Nano. 2018 Apr 24;12(4): 3385-3396.
doi: 10.1021/acsnano.7b08969.
IF=13.903(2019)

PMID: 29553709

Nature Plants. 2016 Dec 22;3: 16206.
doi: 10.1038/nplants.2016.205.
IF=13.297(2019)

PMID: 28005066

Sci Adv. 2018 Oct 24;4(10): eaat6994.
doi: 10.1126/sciadv.aat6994.
IF=12.804(2019)

PMID: 30417089

University of Perugia (Italy)

St. Jude Children Research Hospital (USA)

Utah State University (USA)

Funda??o Universitária de Desenvolvimento (Brazil)

Universidade Católica Portuguesa (Portugal)

Cornell University (USA)

University of Lodz (Poland)

Helmholtz Zentrum München (Germany)

University of Madras (India)

Harvard University (USA)

Universite Libre de Bruxelles (Belgium)

University of Dicle (Turkey)

University of Helsinki (Finland)

Universiti Kebangsaan Malaysia (Malaysia)

More...

Description:

Vorinostat (suberoylanilide hydroxamic acid, SAHA, MK0683) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay. Vorinostat abrogates productive HPV-18 DNA amplification.

Targets:

HDAC

In vitro:

Cancer Res,2001 Dec 1;61(23):8492-7.

The histone deacetylase inhibitor suberoylanilide hydroxamic acid induces differentiation of human breast cancer cells[Pubmed: 11016644]

Histone deacetylase (HDACs) regulate histone acetylation by catalyzing the removal of acetyl groups on the NH(2)-terminal lysine residues of the core nucleosomal histones. Modulation of the acetylation status of core histones is involved in the regulation of the transcriptional activity of certain genes. HDAC activity is generally associated with transcriptional repression. Aberrant recruitment of HDAC activity has been associated with the development of certain human cancers.
METHODS AND RESULTS:
We have developed a class of HDAC inhibitors, such as suberoylanilide hydroxamic acid (SAHA), that were initially identified based on their ability to induce differentiation of cultured murine erythroleukemia cells. Additional studies have demonstrated that SAHA inhibits the growth of tumors in rodents. In this study we have examined the effects of SAHA on MCF-7 human breast cancer cells. We found that SAHA causes the inhibition of proliferation, accumulation of cells in a dose-dependent manner in G(1) then G(2)-M phase of the cell cycle, and induction of milk fat globule protein, milk fat membrane globule protein, and lipid droplets. Growth inhibition was associated with morphological changes including the flattening and enlargement of the cytoplasm, and a decrease in the nuclear:cytoplasmic ratio. Withdrawal of SAHA led to reentry of cells into the cell cycle and reversal to a less differentiated phenotype. SAHA induced differentiation in the estrogen receptor-negative cell line SKBr-3 and the retinoblastoma-negative cell line MDA-468.
CONCLUSIONS:
We propose that SAHA has profound antiproliferative activity by causing these cells to undergo cell cycle arrest and differentiation that is dependent on the presence of SAHA. SAHA and other HDAC inhibitors are currently in Phase I clinical trials. These findings may impact the clinical use of these drugs.

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	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	3.7836 mL	18.9179 mL	37.8358 mL	75.6716 mL	94.5895 mL
5 mM	0.7567 mL	3.7836 mL	7.5672 mL	15.1343 mL	18.9179 mL
10 mM	0.3784 mL	1.8918 mL	3.7836 mL	7.5672 mL	9.4589 mL
50 mM	0.0757 mL	0.3784 mL	0.7567 mL	1.5134 mL	1.8918 mL
100 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.7567 mL	0.9459 mL