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贝利司他 (PXD101)

规格或纯度: ≥98%

CAS编号: 414864-00-9
分子式: C₁₅H₁₄N₂O₄S
分子量: 318.35
PubChem编号: 6918638

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货号 (SKU)	包装规格	是否现货	价格	数量
B126780-10mg	10mg	现货
B126780-50mg	50mg	现货
B126780-250mg	250mg	期货

查看相关系列

histone deacetylase 1 Inhibitor histone deacetylase 2 Inhibitor histone deacetylase 3 Inhibitor histone deacetylase 4 Inhibitor histone deacetylase 5 Inhibitor histone deacetylase 6 Inhibitor histone deacetylase 7 Inhibitor histone deacetylase 8 Inhibitor histone deacetylase 9 Inhibitor

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基本描述

英文别名	Belinostat\|414864-00-9\|PXD101\|866323-14-0\|Belinostat (PXD101)\|Beleodaq\|PXD-101\|(E)-N-hydroxy-3-(3-(N-phenylsulfamoyl)phenyl)acrylamide\|E-Belinostat\|NSC726630\|PXD 101\|PX-105684\|N-HYDROXY-3-(3-PHENYLSULFAMOYLPHENYL)ACRYLAMIDE\|UNII-F4H96P17NZ\|F4H96P17NZ\|PX10
规格或纯度	≥98%
英文名称	Belinostat (PXD101)
生化机理	Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM. Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells. Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase, and increase in G2-M phase. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	卖完停产，不再备货
产品介绍	Belinostat (PXD101)是一种新型的HDAC抑制剂，IC50为27 nM，对抵抗Cisplatin的肿瘤有效。一种新型HDAC抑制剂 Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors. A novel HDAC inhibitor

产品属性

ALogP	1.7

名称和标识符

IUPAC Name	(E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
INCHI	InChI=1S/C15H14N2O4S/c18-15(16-19)10-9-12-5-4-8-14(11-12)22(20,21)17-13-6-2-1-3-7-13/h1-11,17,19H,(H,16,18)/b10-9+
InChi Key	NCNRHFGMJRPRSK-MDZDMXLPSA-N
Canonical SMILES	C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO
Isomeric SMILES	C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)/C=C/C(=O)NO
PubChem CID	6918638
分子量	318.35

数据库链接

PubChem CID	6918638
ChEMBL Ligand	CHEMBL408513
ChEBI	CHEBI:61076
Wikipedia	Belinostat
CAS Registry No.	414864-00-9
DrugBank Ligand	DB05015
RCSB PDB Ligand	5OG
PEP	belinostat
Reactome Reaction	R-HSA-9679787
Reactome Drug	R-ALL-9679789

化学和物理性质

溶解性	DMSO 64 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

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参考文献

1. Qian X, LaRochelle WJ, Ara G, Wu F, Petersen KD, Thougaard A, Sehested M, Lichenstein HS, Jeffers M. (2006) Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies.. Mol Cancer Ther, 5 (8): (2086-95). [PMID:16928830]
2. Buckley MT, Yoon J, Yee H, Chiriboga L, Liebes L, Ara G, Qian X, Bajorin DF, Sun TT, Wu XR et al.. (2007) The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo.. J Transl Med, 5 (13): (49). [PMID:17935615]
3. Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, La Thangue NB, Brown R. (2003) Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101.. Mol Cancer Ther, 2 (8): (721-8). [PMID:12939461]
4. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010) Chemical phylogenetics of histone deacetylases.. Nat Chem Biol, 6 (3): (238-243). [PMID:20139990]
5. Savickiene J, Treigyte G, Valiuliene G, Stirblyte I, Navakauskiene R. (2014) Epigenetic and molecular mechanisms underlying the antileukemic activity of the histone deacetylase inhibitor belinostat in human acute promyelocytic leukemia cells.. Anticancer Drugs, 25 (8): (938-49). [PMID:24800886]
6. Khan N, Jeffers M, Kumar S, Hackett C, Boldog F, Khramtsov N, Qian X, Mills E, Berghs SC, Carey N et al.. (2008) Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors.. Biochem J, 409 (2): (581-9). [PMID:17868033]

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