您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Cabazitaxel
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Cabazitaxel
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cabazitaxel图片
CAS NO:183133-96-2
包装与价格:
包装价格(元)
20 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
RPR-116258A
taxoid XRP6258
TXD 258
卡巴他塞
XRP6258
产品介绍
Cabazitaxel 是一种紫杉烷类的抗肿瘤剂,可用于治疗多西他赛失败后的去势抵抗性转移性前列腺癌。

产品描述

Cabazitaxel is a taxane and antineoplastic agent which is currently used in the therapy of castration-resistant metastatic prostate cancer after failure of docetaxel.

体外活性

使用SF-295和U251人成胶质细胞瘤细胞系,产生原位和皮下鼠异种移植物. Cabazitaxel治疗导致大部分皮下植入的肿瘤完全消退.Cabazitaxel在其它相关模型中也有明显的抗肿瘤活性.Cabazitaxel在小鼠肿瘤异种移植模型 (结肠 C38 和 胰腺 P03)中,引起完全肿瘤消退.此外,Cabazitaxel在原位模型中导致10个U251肿瘤中的4个完全肿瘤消退.

体内活性

Cabazitaxel的平均离体人血浆蛋白结合率为91.6%。Cabazitaxel会被迅速广泛地代谢成多种代谢产物。Cabazitaxel在多个鼠和人的抗性细胞系中都有活性。Cabazitaxel会提高大鼠肝细胞中CYP3A的酶活性。Cabazitaxel在3种结肠癌细胞株(HCT-116,HCT-8和 HT-29) 中显示出高抗肿瘤活性。用相对较低浓度的Cabazitaxel处理四天会产生明显的细胞毒性。

细胞实验

The cytotoxicity of CBX-loaded ANs and free Cabazitaxel (CBX) is evaluated with MTT assay. Cells are seeded onto a 96-well plate at a density of 3000 cells per well and cultured for 24 h. CBX-loaded ANs and free CBX are diluted to predetermined concentrations with PBS and added into each well. Blank AN, AN-ICG and free CBX solvent (a mixture of Tween-80 and anhydrous alcohol) are added as well to different final concentrations. The incubation continued for another 48 hours. 20 μL MTT solutions (5 mg/mL in PBS) are added into each well and cells are incubated for another 4 hours under 37°C. Subsequently the medium is removed and 150 μL dimethyl sulphoxide (DMSO) is added to dissolve the purple formazan salt crystals. Then the absorbance is measured by a microplate reader at 490 nm. The cells treated with medium are evaluated as controls.

Cas No.

183133-96-2

分子式

C45H57NO14

分子量

835.944

别名

RPR-116258A;taxoid XRP6258;TXD 258;卡巴他塞;XRP6258

储存和溶解度

DMSO:93 mg/mL (111.3 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years