Docetaxel, a semisynthetic analog of paclitaxel binds and stablizes tubulin, thus preventing microtubule disassembly, resulting in cell-cycle arrest at the G2/M phase and inducing apoptosis. Docetaxel is known to inhibit the anti-apoptotic gene Bcl2 and induces the expression of cell cycle inhibitor p27. (1)
In in vitro tubule formation assays, taxotere has an IC50 in the low nanomolar range. HUVEC migration assays were more sensitive, with IC50s in the picomolar range in a chemokinetic assay. Furthermore, HUVEC chemotaxis stimulated by either thymidine phosphorylase or vascular endothelial growth factor, was inhibited by Taxotere in the double-digit picomolar range. (2)
Docetaxel has been studied extensively in combination with traditional anti-cancer agents (e.g. gemcitabine) and more recently with newer generation agents such as cisplatin/5-fluorouracil (DCF), everolimus, sunitinib, and antibody therapies. (1, 3)
Technical information:
Chemical Formula: | C43H53NO14 | |
CAS #: | 148408-66-6 | |
Molecular Weight: | 807.88 | |
Purity: | > 98% | |
Appearance: | white | |
Chemical Name: | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate | |
Solubility: | Up to 100 mM in DMSO | |
Synonyms: | Docetaxel, Taxotere |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Nishiyama et al., Docetaxel: its role in current and future treatments for advanced gastric cancer. Gastric Cancer 2009, 12, 132-141. Pubmed ID: 19890692 |
2. | Hotchkiss et al., Inhibition of Endothelial Cell Function in Vitro and Angiogenesis in Vivo by Docetaxel (Taxotere): Association with Impaired Repositioning of the Microtubule Organizing Center. Mol Cancer Ther. 2002, 1, 1191-1200. Pubmed ID: 12479700 |
3. | Fauzee et al., Taxanes: Promising Anti-Cancer Drugs. Asian Pacific J. Cancer Prev. 2011, 12, 837-851. Pubmed ID: 21790213 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.