C-2581 Cabazitaxel, >99%

Synonyms : [RPR-116258] [Taxoid XRP6258] [TXD-258] [XRP-6258]

Related Terms : [Jevtana]

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  • 5 mg
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  • 10 mg
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  • 25 mg
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  • 50 mg
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  • 200 mg
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  • 500 mg
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  • 1 g
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  • 2 g
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  • M.W. 835.93
  • C45H57NO14
  • [183133-96-2]
  • M.I. 14: 10493

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.

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  • 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).
  • Another CAS number previously assigned to cabazitaxel, namely 890654-44-1, has been deleted by CAS and is no longer in use.
  • Cabazitaxel is the active ingredient in the drug product sold under the trade name Jevtana®.  This drug is currently approved in at least one country for use in patients with hormone-refractory metastatic prostate cancer.  NOTE:  THE CABAZITAXEL SOLD BY LC LABORATORIES FOR RESEARCH IS NOT JEVTANA®, AND IS NOT FOR HUMAN USE.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.