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Cabazitaxel Sale

(Synonyms: 卡巴他赛,XRP6258; RPR-116258A; taxoid XRP6258) 目录号 : GC11765

A semisynthetic taxane

Cabazitaxel Chemical Structure

Cas No.:183133-96-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥470.00
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5mg
¥258.00
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10mg
¥450.00
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25mg
¥920.00
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50mg
¥720.00
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100mg
¥1,350.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C 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 experiment [1]:

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.

References:

[1]. Vrignaud P, Sémiond D, Lejeune P, Bouchard H, Calvet L, Combeau C, Riou JF, Commeron A, Lavelle F, Bissery MC. Preclinical antitumor activity of cabazitaxel, a semisynthetic taxane active in taxane-resistant tumors. Clin Cancer Res. 2013 Jun 1;19(11):2973-83.

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.

Chemical Properties

Cas No. 183133-96-2 SDF
别名 卡巴他赛,XRP6258; RPR-116258A; taxoid XRP6258
Canonical SMILES CO[C@H]1C[C@]2([H])[C@](CO2)(OC(C)=O)[C@]3([H])[C@]1(C)C([C@H](OC)C4=C(C)[C@@H](OC([C@H](O)[C@H](C5=CC=CC=C5)NC(OC(C)(C)C)=O)=O)C[C@]([C@H]3OC(C6=CC=CC=C6)=O)(O)C4(C)C)=O
分子式 C45H57NO14 分子量 835.93
溶解度 ≥ 22.3mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.1963 mL 5.9814 mL 11.9627 mL
5 mM 0.2393 mL 1.1963 mL 2.3925 mL
10 mM 0.1196 mL 0.5981 mL 1.1963 mL
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