资料发布时间:2018-10-30 14:50:00 最后更新时间: 2021-06-09 15:17:08
【药品简介】 2003年,美国食品与药物管理局(FDA)快速审批通过了万珂用于多发性骨髓瘤(MM)的临床治疗,2005年,美国FDA和欧洲药物评审局批准万珂用于MM首次复发后的治疗。目前,2010年NCCN(美国国家综合癌症网络)诊疗指南推荐万珂作为多发性骨髓瘤的首选治疗用药。
【适应症状】 硼替佐米,用于多发性骨髓瘤患者的治疗,此患者在使用本品前至少接受过两种治疗,并在最近一次治疗中病情还在进展。 用于复发或难治性套细胞淋巴瘤患者的治疗,此患者在使用本品前至少接受过一种治疗。
【 药品别名 】 硼替佐米 Bortezomib VELCADE
印度硼替佐米(硼替佐米 Bortezomib VELCADE)价格,正品图片,治疗白血病药物, 购买硼替佐米请到印度药房官方网站进行购买 【印度药房大全目录】
【 市场参考价格 】 ¥399.00~590.00
播放/暂停
生物活性
产品描述 |
Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay). |
靶点活性 |
20S proteasome,0.6nM(Ki) |
实验溶液 |
0.5% methylcellulose+0.2% Tween 80: 5 mg/mL |
体外活性 |
The average growth inhibition of 50% (GI50) value for Bortezomib across the entire NCI cell panel was 7 nM. Bortezomib was shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins (IC50: 0.1 μM) [1]. Exposure to bortezomib has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1. Bortezomib also promoted the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response [2]. Bortezomib (0.01-10 μM) treatment caused cell accumulation at the G2-M phase and induced cell apoptotic death in a concentration-dependent manner. The slower mobility of the Bcl-2 band corresponded to the phosphorylation of the Bcl-2 protein and could be seen in the cells exposed to 0.01–0.05 μM Bortezomib for 24 h. Another slower band could be discerned, which corresponded to a superphosphorylated form of Bcl-2, and was detected when cells were exposed to higher concentrations of Bortezomib (0.1–10 μM) for 24 h [3]. |
体内活性 |
On 4 consecutive days, Bortezomib (1.0 mg/kg) was administered (in 10 μl) into established PC-3 tumors, and results showed a dramatic decrease in tumor burden. In addition to the large decrease in tumor volume (70%), two of five mice (40%) had no detectable tumors at the end of the study [1]. The mice were injected s.c. with 3 x 10(7) RPMI-8226 myeloma cells. When tumors became measurable, mice were assigned to treatment groups receiving Bortezomib 0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, or 1.0 mg/kg twice weekly via the tail vein, or to control groups receiving the vehicle only. Significant inhibition of tumor growth, even with some complete tumor regression, was observed in Bortezomib-treated mice. The median overall survival was also significantly prolonged compared with controls [4]. |
激酶实验 |
Kinetic Methods: In a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL−10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates. |
细胞实验 |
The inhibitory effect of Bortezomib on cell growth is assessed by measuring MTT dye absorbance of the cells. Cells from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer. (Only for Reference) 细胞系: Human multiple myeloma cells line U266 |
动物实验 |
动物模型:Human plasmacytoma xenografts RPMI 8226 |
化学信息
分子量 |
384.24 |
分子式 |
C19H25BN4O4 |
CAS |
179324-69-7 |
溶解度 |
DMSO: 71 mg/mL (184.8 mM) Ethanol: <1 mg/mL Water: <1 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 2.603 ml | 13.013 ml | 26.025 ml |
5 mM | 0.521 ml | 2.603 ml | 5.205 ml |
10 mM | 0.26 ml | 1.301 ml | 2.603 ml |
50 mM | 0.052 ml | 0.26 ml | 0.521 ml |
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