Rapamycin
R-900
10x10 μg 0.1 mg 0.5 mg 1mg 5x1mg
Brand
Description
Rapamycin
Immunosuppresant
| Product#: | R-900 |
| Sizes: |
| 10 x 10 mg |
| 0.1 mg |
| 0.5 mg |
| 1 mg |
| 5 x 1 mg |
| M.W.: | 914.2 |
| CAS No.: |
53123-88-9
|
| Structure: |
| . |
 |
| Purity: | >99% |
| Bioassay: |
| The biological activity was tested to confirm the ability of Rapamycin to inhibit the proliferation of WEHI B lymphocyte cells. |
 |
| WEHI B lymphocyte cells were treated with different concentrations of Rapamycin for 4 days; the number of live cells was measured by XTT cell proliferation assay kit, normalized to the control (100 %) and plotted against drug concentration. |
| References: |
|
1. |
Cardenas, M. et al. (1994) Perspect. Drug Discov. Des. 2, 103.
|
|
2. |
Albers, M. et al. (1993) J. Biol. Chem. 268, 22825. |
|
3. |
Aimee L. Edinger, et al. (2003) Cancer Res. 63, 8451. |
|
4. |
Hajime Hosoi. et al. (1999) Cancer Res. 59, 886. |
|
5. |
Shile Huang. et al. (2001) Cancer Res. 61, 3373. |
|
6. |
Liu, J. et al. (1991) Cell 66, 807. |
|
7. |
Fruman, D. A. et al. (1992) Proc. Natl. Acad. Sci. U. S. A. 89. 3686
|
Rapamycin is a natural macrocyclic antibiotic with both antifungal and immunosuppressive activities.1 In mammalian T-lymphocytes, Rapamycin blocks the signal transduction pathway initiated by interleukin-2.2
Rapamycin has also shown promising anticancer activities in preclinical and clinical studies,3 acting as an antiproliferative agent in vascular, endothelial and smooth muscle cells. It also induced apoptosis in two rhabdomyosarcoma cell lines.4
Together with FKBP12, Rapamycin creates a toxic complex that irreversibly inhibits mTOR kinase- a downstream effector of the phosphatidylinositol 3-kinase/Akt signaling pathway.3,5 By the use of this mechanism Rapamycin arrests the progression of G
-phase T-cells to S phase.6 The FKBP12 –Rapamycin complex also inhibits the Ca2+-calmodulin-regulated protein serine-threonine phosphatase, Calcineurin.7
Application
Reactivity
