Cabazitaxel,183133-96-2

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产品名称：Cabazitaxel

产品别名：卡巴他赛

英文别名：XRP6258;RPR-116258A;taxoid XRP6258;TXD 258

靶点：Microtubule

CAS：183133-96-2

纯度：98% min

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Cabazitaxel(XRP6258; RPR-116258A)是天然的taxoid 10-deacetylbaccatin III半合成衍生物，具有抗肿瘤活性。

溶解性：DMSO Solubility: 100 mg/mL (119.62 mM)

体外研究：

Cabazitaxel increases CYP3A enzyme activities in rat hepatocytes. The mean ex-vivo human plasma protein binding of Cabazitaxel is 91.6%. Cabazitaxel is rapidly and extensively metabolised in numerous metabolites. Cabazitaxel demonstrates activity in several murine and human resistant cell lines. With a 4-day exposure to cabazitaxel, cytotoxicity is noted with relatively low cabazitaxel concentrations. Cabazitaxel shows high antitumor activity in 3 human colorectal cell lines (HCT-116, HCT-8, and HT-29).

体内研究：In accompanying models, Cabazitaxel is noted to have significant antitumor activity. In murine tumor xenografts (colon C38 and pancreas P03), Cabazitaxel elicites complete tumor regressions. Using SF-295 and U251 human glioblastoma cell lines, both orthotopic and subcutaneous murine xenografts are generated. Cabazitaxel treatment leads to complete regression in the majority of subcutaneously implanted tumors. Furthermore, in orthotopic models, Cabazitaxel leads to complete tumor regression in 4 out of 10 U251 tumors.

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