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Belinostat 贝利司他

目录号 M1670 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


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。

Belinostat结构式

别名:PXD101; PX105684

规格 价格 库存状态
Free Sample (0.5-1 mg)  ¥ 0 中国库存现货
10mM*1mL in DMSO ¥ 720 中国库存现货
5mg ¥ 450 中国库存现货
10mg ¥ 675 中国库存现货
50mg ¥ 1575 中国库存现货
100mg ¥ 2340 中国库存现货
200mg ¥ 3600 中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

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。Belinostat抑制肿瘤细胞生长(包括A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3,及HS852),IC50为0.2到0.66 μM。Belinostat 作用于A2780/cp70 和2780AD细胞时活性很低, 这两个细胞是抗cisplatin和doxorubicin的A2780细胞衍生的。Belinostat通过PARP分裂和组蛋白H3/H4的乙酰化而诱导细胞凋亡。

实验参考
体外实验*
细胞系 A2780, A2780/cp70, CALU-3, MCF7, PC3, HS852, HT29 and HCT116 cell lines
方法 Cytotoxicity Assay.
Drug sensitivity was determined by a clonogenic assay (13). Briefly, cells were plated in 5 ml of medium at a density of 8 × 104 cells/25 cm2 flask and allowed to attach and grow for 48 h. Cells were exposed to drug (five concentrations from 0.016 to 10 μM) for 24 h. The medium was removed, and 1 ml of trypsin/EDTA was added to each flask. Once the cells had detached, 1 ml of medium was added, the cells were resuspended, and those from the control untreated flask were counted. Cells were diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks were diluted and plated as for the control flasks. Dishes were incubated for 10–15 days at 37°C. Cells were washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 (mean ± SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells.
浓度 0.016 ~ 10 μM
处理时间 24 h

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

体内实验*
动物模型 A2780, A2780/cp70 and HCT116 tumor-bearing mice model
配制 dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10%
剂量 a single injection of 40 mg/kg
给药处理 i.p.

*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

化学性质
分子量 318.35
分子式 C15H14N2O4S
CAS号 414864-00-9
溶解性(25°C) DMSO 60 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.1412 mL 15.706 mL 31.412 mL
5 mM 0.6282 mL 3.1412 mL 6.2824 mL
10 mM 0.3141 mL 1.5706 mL 3.1412 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Yeo W, et al. J Clin Oncol. Epigenetic therapy using belinostat for patients with unresectable hepatocellular carcinoma: a multicenter phase I/II study with biomarker and pharmacokinetic analysis of tumors from patients in the Mayo Phase II Consortium and the Cancer Therapeutics Research Group.

[2] Dizon et al. Int J Gynecol Cancer. Phase II activity of belinostat (PXD-101), carboplatin, and paclitaxel in women with previously treated ovarian cancer.

[3] Dovzhanskiy et al. BMC Cancer. Experimental in vivo and in vitro treatment with a new histone deacetylase inhibitor belinostat inhibits the growth of pancreatic cancer.

[4] Dizon et al. Gynecol Oncol. A phase II evaluation of belinostat and carboplatin in the treatment of recurrent or persistent platinum-resistant ovarian, fallopian tube, or primary peritoneal carcinoma: a Gynecologic Oncology Group study.

[5] Gravina et al. Int J Oncol. Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models.

[6] Molife et al. Expert Opin Investig Drugs. Belinostat: clinical applications in solid tumors and lymphoma.

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