| Description |
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor[1].
|
| Related Catalog |
|
| Target |
PI3K, mTOR[1]
|
| In Vitro |
NVP-BBD130 (1 μM; 72 h) blocks proliferation of melanoma cells, arrests cell cycle at G1 phase in A2058 cells but not C32 cells[1]. Cell Proliferation Assay[1] Cell Line: Melanoma cells Concentration: 1 μM Incubation Time: 3 days Result: Showed a long-term effect on melanoma cell proliferation. Western Blot Analysis[1] Cell Line: A2058 and C32 cells Concentration: 1 μM Incubation Time: 0, 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h Result: Decreased phosphorylation of PKB/Akt, whereas the phosphorylation status of MAPK was not affected. Down-regulated the expression of cyclin D1, induced p27Kip1 expression in A2058 cells. Cell Cycle Analysis[1] Cell Line: A2058 cells Concentration: 1 μM Incubation Time: 3 days Result: Resulted in a complete arrest of most tumor cells in G1.
|
| In Vivo |
NVP-BBD130 (40 mg/kg; p.o.; daily for 2 weeks) efficiently attenuates tumor growth at primary and lymph node metastatic sites with no obvious toxicity, and is well tolerant in B16BL6 mouse melanoma model[1]. Animal Model: C57BL6 mice, syngeneic B16BL6 mouse melanoma model[1] Dosage: 40 mg/kg Administration: Oral administration, daily for 2 weeks Result: Reduced primary tumor size, showed a significant reduction in the size of the cervical lymph node metastasis.
|
| References |
[1]. Marone R, et al. Targeting melanoma with dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors. Mol Cancer Res. 2009 Apr;7(4):601-13.
|
