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| 规格： | 10 mM * 1 mL | 产品价格： | ￥920.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥550.0 |
| 规格： | 5 mg | 产品价格： | ￥900.0 |
| 规格： | 10 mg | 产品价格： | ￥1500.0 |
| 规格： | 50 mg | 产品价格： | ￥4500.0 |
| 规格： | 100 mg | 产品价格： | ￥7500.0 |
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GNE-617
CAS No. : 1362154-70-8
MCE 国际站：GNE-617
产品活性：GNE-617是新型特异的Nampt抑制剂，在A549细胞中IC50为18.9nM。
研究领域：Metabolic Enzyme/Protease
作用靶点：NAMPT
In Vitro: The activity ofGNE-617 hydrochloride is evaluated on a panel 53 non-small cell lung cancer (NSCLC) cell lines in the presence or absence of 10 μM nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cell.The majority of cell lines exhibit a steep dose response to GNE-617 when evaluated by decrease in ATP or total nucleic acid, and the cytotoxicity is completely rescued by simultaneous addition of nicotinic acid. The majority of the cell lines tested have IC50 values below 100 nM, with approximately half with IC50 values less than 10 nM.
In Vivo: In rats, GNE-617 (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity.
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