853910-61-9
853910-61-9 structure
- Name: BBD130
- Chemical Name: 2-methyl-2-[4-[3-methyl-2-oxo-8-(2-pyridin-3-ylethynyl)imidazo[4,5-c]quinolin-1-yl]phenyl]propanenitrile
- CAS Number: 853910-61-9
- Molecular Formula: C28H21N5O
- Molecular Weight: 443.499
- Catalog: Signaling Pathways PI3K/Akt/mTOR mTOR
- Create Date: 2016-10-30 02:13:44
- Modify Date: 2024-01-16 11:57:47
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NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor[1].
| Name | 2-methyl-2-[4-[3-methyl-2-oxo-8-(2-pyridin-3-ylethynyl)imidazo[4,5-c]quinolin-1-yl]phenyl]propanenitrile |
|---|---|
| Synonyms |
2-Methyl-2-{4-[3-methyl-2-oxo-8-(3-pyridinylethynyl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile
2-methyl-2-{4-[3-methyl-2-oxo-8-(pyridin-3-ylethynyl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]phenyl}propanenitrile Benzeneacetonitrile, 4-[2,3-dihydro-3-methyl-2-oxo-8-[2-(3-pyridinyl)ethynyl]-1H-imidazo[4,5-c]quinolin-1-yl]-α,α-dimethyl- |
| 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 |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 693.7±65.0 °C at 760 mmHg |
| Molecular Formula | C28H21N5O |
| Molecular Weight | 443.499 |
| Flash Point | 373.3±34.3 °C |
| Exact Mass | 443.174622 |
| PSA | 76.50000 |
| LogP | 3.23 |
| Vapour Pressure | 0.0±2.2 mmHg at 25°C |
| Index of Refraction | 1.732 |