Cabazitaxel

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本试剂(Cabazitaxel)
仅供科研实验使用,不得用于其他用途！

简介：
货 号：C-2581
名 称：Cabazitaxel
别 名：Cabazitaxel
C A S ：183133-96-2
分子量：835.93
分子式：C45H57NO14
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; soluble in ethanol at 50 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-2 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.
文 献：Cabazitaxel, also known as XRP-6258, is a second-generation semi-synthetic derivative of paclitaxel, a natural taxoid microtubule inhibitor. Paller, C.J. and Antonarakis, E.S. "Cabazitaxel: a novel second-line treatment for metastatic castration-resistant prostate cancer." Drug Des. Devel. Ther. 5: 117-124 (2011). In preclinical studies, cabazitaxel was shown to have antitumor activity in a variety of docetaxel-refractory in vitro and in vivo models. Bissery, M-C., et al. "Preclinical evaluation of TXD258, a new taxoid." Proceedings of the American Association for Cancer Research Abstract 411364 (2000). Vrignaud, P., et al. "In vivo efficacy of TXD258, a new taxoid, against human tumor xenografts." Proceedings of the American Association for Cancer Research Abstract 411365 (2000). 755 participants with metastatic castration-resistant prostate cancer who had received previous hormone therapy were treated with prednisone daily, and were randomly allocated to treatment groups (377 mitoxantrone and 378 cabazitaxel). Median survival was 15.1 months in the cabazitaxel group and 12.7 months in the mitoxantrone group. Median progression-free survival was 2.8 months in the cabazitaxel group and 1.4 months in the mitoxantrone group. de Bono, J.S., et al. "Prednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: a randomised open-label trial." Lancet 376: 1147-1154 (2010). When compared with docetaxel and paclitaxel, cabazitaxel was reported to have poor affinity for the ATP-dependent drug efflux pump, P-glycoprotein 1 (P-gp), and greater penetration of the blood-brain barrier. Mita, A.C., et al. "Phase I and pharmacokinetic study of XRP6258 (RPR 116258A), a novel taxane, administered as a 1-hour infusion every 3 weeks in patients with advanced solid tumors." Clin. Cancer Res. 15: 723-730 (2009). Brain uptake of cabazitaxel was increased when concentrations exceeded 11 µM and the saturation was found to be at 13 µM, suggesting the role of a critical transporter (that is, P-gp) in transporting cabazitaxel across the blood-brain barrier upon a certain threshold. Cisternino, S., 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. 138: 1367-1375 (2003).