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/ Cabazitaxel

卡巴他赛 /Cabazitaxel {[allProObj[0].p_purity_real_show]}

货号：A209461 同义名： 卡巴他塞 / XRP6258;RPR-116258A

Cabazitaxel是从天然药物 10-脱乙酰巴卡亭 III 半合成的，具有潜在的抗肿瘤活性。

Cabazitaxel 化学结构 CAS号：183133-96-2
Cabazitaxel 化学结构
CAS号：183133-96-2
Cabazitaxel 3D分子结构
CAS号：183133-96-2
Cabazitaxel 化学结构 CAS号：183133-96-2
Cabazitaxel 3D分子结构 CAS号：183133-96-2
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Cabazitaxel 纯度/质量文件 产品仅供科研

货号：A209461 标准纯度： {[allProObj[0].p_purity_real_show]}
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Cabazitaxel 生物活性

描述 Microtubules are the main constituent of mitotic apparatus in all eukaryotic cells, thus make it become an important pharmacological target for the treatment of tumor[1]. Cabazitaxel can bound to unfractionated microtubules with KD 7.4 μM (measured by [14C]-labled binding stoichiometries). Cabazitaxel is used as a microtubule-targeted cancer chemotherapeutic agent for treatment of metastatic castrationresistant prostate cancer after failure of docetaxel treatment. Compared with docetaxel, cabazitaxel can suppress microtubule dynamic instability significantly more potently in the presence of βIII-tubulin than in its absence. This was supported by the study of βIIItubulin-deleted microtubule assembly experiment orβIII-tubulin-knockdown MCF7 cells. Also, it was found that mitotic arrest IC50 for cabazitaxel was significantly more potent in control-transfected cells (8 nM) than in βIII-tubulin- knockdown cells (18 nM, a 2.3-fold difference). Thus, The selective potency of cabazitaxel on βIII-tubulin-containing level may explain the superior anti-tumor efficacy of cabazitaxe in tumors overexpressing βIII-tubulin [a]. Specifically, cabazitaxel has the ability to cross the blood–brain barrier[2]. Cabazitaxel is approved for use in combination with prednisone for treatment of metastatic hormone refractory prostate cancer previously treated with a docetaxel-containing regimen (see in FDA net).
作用机制 Cabazitaxel can bind and stabilize microtubules and suppress microtubule dynamic instability significantly more potently in the presence of βIII-tubulin than in its absence[3].

Cabazitaxel 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A431 cells Growth inhibition assay Growth inhibition of human A431 cells by MTT assay, IC50=1.48 nM 24405702
human A549 cells Growth inhibition assay Growth inhibition of human A549 cells by MTT assay, IC50=1.48 nM 24405702
human DU145 cells Growth inhibition assay Growth inhibition of human DU145 cells by MTT assay, IC50=1.43 nM 24405702
human HeLa cells Growth inhibition assay Growth inhibition of human HeLa cells by MTT assay， IC50=1.8 nM 24405702

Cabazitaxel 动物研究

Dose Mice (i.p.): min = 9 mg/kg[4], max = 33 mg/kg[5]
Administration i.p.
Pharmacokinetics
Animal Rats[6]
Dose 2.5 mg/kg
Administration i.v.
Cmax 477 ng/ml
Tmax 1 h
Tlast 10 h
CL 4.79 L/(h·kg)
Vss 22.7 L/kg
AUC 522 ng·h/ml
T1/2z 10.1 h

Cabazitaxel 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03419442 - Not yet recruiting February 28, 2019 United States, New Jersey ... 展开 >> US database Not yet recruiting Whippany, New Jersey, United States, 07981 收起 <<
NCT01379339 Squamous Cell Carcinoma of the... 展开 >> Head and Neck 收起 << Phase 1 Completed - United States, New York ... 展开 >> Icahn School of Medicine at Mount Sinai New York, New York, United States, 10029 收起 <<
NCT01447225 Solid Tumors Phase 1 Completed - United States, Indiana ... 展开 >> Lafayette, Indiana, United States, 47905 United States, New York Buffalo, New York, United States, 14263 United States, Ohio Cincinnati, Ohio, United States, 45267 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19111 France Villejuif, France 收起 <<

Cabazitaxel 参考文献

[1]Fong KW, Leung JW, et al. MTR120/KIAA1383, a novel microtubule-associated protein, promotes microtubule stability and ensures cytokinesis. J Cell Sci. 2013 Feb 1;126(Pt 3):825-37.

[2]Cisternino S, Bourasset F, et al. Nonlinear accumulation in the brain of the new taxoid TXD258 following saturation of P-glycoprotein at the blood-brain barrier in mice and rats. Br J Pharmacol. 2003 Apr;138(7):1367-75.

[3]Smiyun G, Azarenko O, et al. βIII-tubulin enhances efficacy of cabazitaxel as compared with docetaxel. Cancer Chemother Pharmacol. 2017 Jul;80(1):151-164.

[4]Girard E, Ditzler S, et al. Efficacy of cabazitaxel in mouse models of pediatric brain tumors. Neuro Oncol. 2015 Jan;17(1):107-15.

[5]van Soest RJ, de Morrée ES, et al. Targeting the Androgen Receptor Confers In Vivo Cross-resistance Between Enzalutamide and Docetaxel, But Not Cabazitaxel, in Castration-resistant Prostate Cancer. Eur Urol. 2015 Jun;67(6):981-985.

[6]201023s000PharmrR

Cabazitaxel 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.20mL

0.24mL

0.12mL

5.98mL

1.20mL

0.60mL

11.96mL

2.39mL

1.20mL

Cabazitaxel 技术信息

CAS号183133-96-2
分子式C45H57NO14
分子量 835.932
别名 卡巴他塞 ;XRP6258;RPR-116258A;dimethoxydocetaxel US brand name: Jevtana.;axoid XRP6258;TXD 258;taxoid XRP6258
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(125.61 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

Tags: Cabazitaxel | XRP6258;RPR-116258A;axoid XRP6258;TXD 258;taxoid XRP6258 | 卡巴他塞 | Anti-tumor | Microtubule/Tubulin | AmBeed-信号通路专用抑制剂 | Cabazitaxel 纯度/质量文件 | Cabazitaxel 生物活性 | Cabazitaxel 细胞研究 | Cabazitaxel 动物研究 | Cabazitaxel 临床数据 | Cabazitaxel 参考文献 | Cabazitaxel 实验方案 | Cabazitaxel 技术信息

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