17-AAG
- 貨號 Cat. No.
- A-580
- 規格 Size
- 0.1 mg 5x0.1mg
Description
17-AAG
An Anticancer Antibiotic
| Product#: | A-580 |
| Sizes: |
| 0.1 mg |
| 5 x 0.1 mg |
| M.W.: | 585.7 |
| CAS No.: | [75747-14-7] |
| Structure: |
| . |
 |
| Purity: | >99% |
| Bioassay: |
The biological activity was tested to confirm the ability of 17AAG to inhibit the growth of tumor cell lines.
|
 | Hela cells were grown in presence of different concentrations of 17AAG. The cell quantity was measured using the tryphan blue method after 4 days. The cell quantity versus 17AAG concentrations is presented in the figure. |
| References: |
1. | Clarke, P.A. et al. (2000) Oncogene 19, 4125. |
2. | Basso, A.D., et al. (2002) Oncogene 21, 1159. |
3. | Schnur, R.C., et al. (1995) J. Med. Chem. 38, 3806. |
4. | Nguyen, D.M. et al. (2001) Ann. Thorac. Surg. 72, 371. |
5. | Yang, J. et al. (2001) Cancer Res. 60, 4010. |
6. | Nimmanapalli, R. et al. (2001) Cancer Res. 61, 1799. |
7. | Neckers, L. (2002) Clin Cancer Res. 8, 962. |
8. | Bagatell, R. et al. (2001) Clin. Cancer Res. 7, 2076. |
9. | Chiosis, G. et al. (2003) Mol. Cancer Ther. 2, 123-129 |
17-AAG is a less toxic and more stable derivative of the antibiotic Geldanamycin. It binds to Hsp90 and regulates its function.1 Hsp90 regulates the physiology of cells exposed to environmental stress and in maintaining the malignant phenotype of tumor cells. 17-AAG induces apoptosis and displays anti-tumor effects in tumor cells. 17-AAG depletes cancer cells of erbB-1, erbB-2, Raf-1, and Akt and hence inhibits the Ras/Raf/MEK and PI3-kinase signaling pathways.2,3 It also downregulates vascular endothelial growth factor (VEGF) expression.4 17AAG is currently in phase I clinical trial in several centers worldwide.5-8 Preliminary data obtained from these trials demonstrate that anti tumor activity is achieved at concentrations below the maximum tolerated dose.9