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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Cabazitaxel 是天然紫杉类化合物 10-deacetylbaccatin III 的半合成衍生物,具有潜在的抗肿瘤活性。

Cell lines

P-glycoprotein-expressing cell lines with chemotherapy resistance

Preparation method

The solubility of this compound in DMSO is >22.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

96 hrs

Applications

Cabazitaxel showed antiproliferative activity by decreasing the lag time of tubulin assembly and the rate of cold-induced microtubule depolymerization. In P-glycoprotein-expressing cell lines with resistance to taxanes (P388/TXT, Calc18/TXT and HL60/TAX) or to other chemotherapy agents (P388/DOX, P388/VCR and KBV1), Cabazitaxel was more effective than Docetaxel (IC50 ranges: Cabazitaxel, 0.013 ~ 0.414 mM; Docetaxel, 0.17 ~ 4.01 mM). Cabazitaxel showed relatively lower resistance factors (2 ~ 10) that those of Docetaxel (5 ~ 59).

Animal models

Mice bearing Docetaxel-sensitive MA16/C adenocarcinomas

Dosage form

64.5, 40, 24.8 or 15.4 mg/kg; i.v.

Applications

In mice bearing Docetaxel-sensitive MA16/C adenocarcinomas, Cabazitaxel showed significant anti-tumor activity, inducing CRs in 80% of mice and displaying a log cell kill of 3.7 at the HNTD of 40 mg/kg. The maximum drug concentration in tumors was reached 15 mins after dosing. At 48 hrs after dosing, the concentration of Cabazitaxel in tumors was 40-fold higher than that in plasma.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity.

The cytotoxicity of cabazitaxel (100 μg/mL) on 4T1 cells without irradiation is 70.8%. Cabazitaxel (100 μg/mL) exhibits a concentration-dependent antiproliferation effect, with the antiproliferative activity of 56.2%[1].

Cabazitaxel (10 mg/kg, i.v.) has certain toxicity to liver and kidney but it can be avoided by integrated into Ans. The body weights of mice treated with AN-ICG-CBX and AN-CBX have a slightly decrease, while body weights of the free CBX group significantly decrease compared to the control group[1].

References:
[1]. Tai X, et al. Cabazitaxel and indocyanine green co-delivery tumor-targeting nanoparticle for improved antitumor efficacy and minimized drug toxicity. J Drug Target. 2016 Sep 9:1-29.
[2]. Gdowski AS, et al. Bone-targeted cabazitaxel nanoparticles for metastatic prostate cancer skeletal lesions and pain. Nanomedicine (Lond). 2017 Sep;12(17):2083-2095.