Docetaxel
- 貨號 Cat. No.
- D-800
- 規格 Size
- 5 mg 5x5 mg 25 mg
Description
Docetaxel
| Product#: | D-800 |
| Sizes: |
| 5 mg |
| 5 x 5 mg |
| 25 mg |
| M.W.: | 807.89 |
| Structure: |
 |
| Purity: | >98% |
| Bioassay: |
| Docetaxel prevents cell division and induces the formation of microtubule bundles in the cell cytoplasm of Human Umbilical Vein Endothelial cells (HUVECs). |
 |
| HUVECs were treated with vehicle (A) or with 10nM (B) and 100 nM (C) Docetaxel. After 22h of treatment, the cells were fixed with 4% PFA and probed with anti b-tubulin followed by a Rodamine-conjugated secondary antibody (2) and DNA was stained with Hoechst 33342 (1). Image (3) of each treatment is the digital overlay of images (1) and (2). Picture (B) presents a multi-nuclear cell caused by low concentrations of Docetaxel (white arrows) and in Picture (C) the white arrow shows microtubule bundles caused by higher concentrations of Docetaxel. |
| References: |
1. | Wani, M.C. et al. (1971) J. Am. Chem. Soc. 93, 2325. |
2. | Holton, R. A. et al. (1995) In: M. Suffness (ed.), Taxol Science and Applications, pp. 97?12. Boca Raton, FL: CRC Press. |
3. | Schiff, P.B. et al. (1979) Nature, 277, 665. |
4. | Parness, J. and Horwitz, S. B. (1981) J. Cell Biol. 91, 479. |
5. | Ringel, I. and Horwitz, S. B. (1989) J. Natl. Cancer Inst. 83, 288. |
6. | Gueritte-Voegelein, F. et al. (1991) J. Med. Chem. 34, 992. |
7. | Pazdur, R. et al. (1993) Cancer Treat Rev. 19, 351. |
8. | Rowinsky, E. K. and Tolcher, A. W. Antimicrotubule agents. In: V. T. Devita, Jr., S. Hellman, and S. A. Rosenberg (eds.), (2001) Cancer Principles and Practice, pp. 431. Philadelphia: Lippincott Williams and Wilkins. |
9. | Hagisawa, S. et al. (1999) Med. Electron Microsc. 32, 167. |
10. | Yoshida, K. et al. (2001) Semin Oncol. 4, 3. |
11. | Horwitz, S. B. (1992) Trends Pharmacol. Sci. 13, 134. |
12. | Moos, P. J. and Fitzpatrick, F. A. (1998) Proc. Natl. Acad. Sci. U.S.A. 95, 3896. |
13. | Rodi, D. J et al. (1999) J. Mol. Biol. 285, 197. |
Docetaxel (DTX) is a semi-synthetic taxane, derived from Paclitaxel, which was originally isolated from the inner bark of the Pacific Yew tree (Taxus brevifolia). Docetaxel is prepared by estertification of Paclitaxel (Taxol) side chain to 10-deacetyl baccatin III (10-DAB). On the basis of photoaffinity labeling and crystallographic analyses, Docetaxel was shown to inhibit the function of tubulin by binding to a similar, highly defined region within b-tubulin.1-6 Docetaxel disturbs the dynamic equilibrium of microtubules by inhibiting the net removal of tubulin dimers from the polymer end. The resulting microtubule/docetaxel complex does not have the ability to disassemble. At stoichiometric concentrations, Docetaxel enhances microtubule assembly.7,8
Because of Docetaxel's ability to act as a microtubule stabilizer, it was shown to be an anti-mitotic, apoptosis inducer and anti-neoplastic agent.7,9,10 Some studies indicate that this activity of taxanes in general and Docetaxel in particular, may originate in part, from the induction of genetic encoding of transcription factors with tumor suppressant effects as well as enzymes governing proliferation, apoptosis, inflammation and other anti-proliferative factors.11-13