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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 ![]() |
|
| 英文别名 | E-Belinostat | s1085 | N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]-2-propenamide | NSC726630 | NSC-726630 | CCG-208758 | MLS006011091 | N-hydroxy-3-(3-(phenylsulfamoyl)phenyl)prop-2-enamide | PXD101;PX105684 | (E)-N-Hydroxy-3-(3-phenylsulfamoyl-phenyl)-acryla |
|---|---|
| 规格或纯度 | Moligand™, ≥98% |
| 英文名称 | Belinostat (PXD101) |
| 生化机理 | 贝利诺司他(Belinostat,PXD101)是一种新型 HDAC 抑制剂,IC50 为 27 nM。贝立诺他能抑制肿瘤细胞(A2780、HCT116、HT29、WIL、CALU-3、MCF7、PC3 和 HS852)的生长,IC50 为 0.2-0.66 μM。PD101 对 A2780/cp70 和 2780AD 细胞的活性较低。贝利诺司他可抑制膀胱癌细胞的生长,尤其是在 5637 细胞中,其表现为 G0-G1 期累积,S 期减少,G2-M 期增加。贝利诺司他还能增强卵巢癌细胞株的微管蛋白乙酰化。最近的一项研究表明,贝利诺司他在 TGF-β 信号依赖性机制中激活了蛋白激酶 A,并降低了存活素 mRNA。 |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 组蛋白去乙酰化酶 1 抑制剂;组蛋白去乙酰化酶 2 抑制剂;组蛋白去乙酰化酶 3 抑制剂;组蛋白去乙酰化酶 4 抑制剂;组蛋白去乙酰化酶 5 抑制剂;组蛋白去乙酰化酶 6 抑制剂;组蛋白去乙酰化酶 7 抑制剂;组蛋白去乙酰化酶 8 抑制剂;组蛋白去乙酰化酶 9 抑制剂 |
| 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. |
| 纯度 | ≥98% |
| ALogP | 1.7 |
|---|
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| PubChem SID | 504764377 |
|---|---|
| 分子类型 | 小分子 |
| IIUPAC Name | (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide |
| 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 |
| 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 |
| 分子量 | 318.35 |
| Reaxy-Rn | 18546675 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18546675&ln= |
| 溶解性 | DMSO 64 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
|---|---|
| 分子量 | 318.300 g/mol |
| XLogP3 | 1.700 |
| 氢键供体数Hydrogen Bond Donor Count | 3 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 5 |
| 精确质量Exact Mass | 318.067 Da |
| 单同位素质量Monoisotopic Mass | 318.067 Da |
| 拓扑极表面积Topological Polar Surface Area | 104.000 Ų |
| 重原子数Heavy Atom Count | 22 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 492.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 1 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 1 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 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 (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] |