Belinostat
货号：
IB0750
品牌：
Jinpan
暂无详情
产品简介
| 别名 | 苯林若斯特;Beleodaq; PXD101; NSC726630; PX-105684 |
| 英文名称 | Belinostat |
| CAS | 414864-00-9 |
| 分子式 | C15H14N2O4S |
| 分子量 | 318.35 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | PXD101 is a novel hydroxamate-type inhibitor of histone deacetylase activity that inhibits histone deacetylase activity in HeLa cell extracts with an IC(50) of 27 nM and induces a concentration-dependent (0.2-5 micro M) increase in acetylation of histone H4 in tumor cell lines.[1] |
| In Vitro | PXD101 is cytotoxic in vitro in a number of tumor cell lines with IC(50)s in the range 0.2-3.4 micro M as determined by a clonogenic assay and induces apoptosis. [1] |
| In Vivo | Treatment of nude mice bearing human ovarian and colon tumor xenografts with PXD101 (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with PXD101.[1] |
| 激酶实验 | For activity assays, the reaction was carried out in a total volume of 150 μl of buffer [60 mm?Tris (pH 7.4) containing 30% glycerol] containing 2 μl of cell extract and, where used, 2 μl of PXD101. The reaction was started by the addition of 2 μl of [3H]labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples were incubated at 37°C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12?m?final concentrations, respectively). Released [3H]acetate was extracted into 750 μl of ethyl acetate, and samples were centrifuged at 12,000 ×?g?for 5 min. The upper phase (600 μl) was transferred to 3 ml of scintillation fluid and counted.[1] |
| SMILES | O=C(NO)/C=C/C1=CC=CC(S(=O)(NC2=CC=CC=C2)=O)=C1 |
| 靶点 | HDAC inhibitor |
| 细胞实验 | For the human tumor xenograft studies, monolayer cultures were harvested with trypsin/EDTA (0.25%/1 mm?in PBS) and resuspended in PBS. About 107?cells were injected s.c. into the right flank of athymic nude mice (CD1?nu/nu?mice from Charles River). After 10–15 days when the mean tumor diameter was ≥0.5 cm, animals were randomized into groups of six for experiments. PXD101 was dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% and was administered i.p. at the times specified. This formulation gave sufficient solubility for doses of ≤40 mg/kg. Mice were weighed daily, and tumor volumes were estimated by caliper measurements assuming spherical geometry (volume =?d3?× π/6). Mice were also observed daily for any changes in behavior or condition according to the Morton and Griffiths scoring system (14). Significant differences between groups were identified by ANOVA, and the significance level of individual differences was determined by Student’s?t?test.[1] |
| 数据来源文献 | [1] Plumb JA, et al. Mol Cancer Ther, 2003, 2(8), 721-728. |
| 规格 | 10mg 50mg |
是一种新型HDAC抑制剂。
