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2070014-99-0

中文名称 GNE-617 (hydrochloride)
英文名称 GNE-617 (hydrochloride)
CAS 2070014-99-0
分子式 C??H??ClF?N?O?S
分子量 463.88
MOL 文件 2070014-99-0.mol
2070014-99-0 结构式 2070014-99-0 结构式

基本信息

中文别名
NAMPT抑制剂
英文别名
GNE-617 (hydrochloride)

物理化学性质

形态Solid
颜色White to off-white
GNE-617 (hydrochloride)价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-15766AGNE-617 (hydrochloride)
GNE-617 hydrochloride
2070014-99-02mg550元
2024/04/30HY-15766AGNE-617 (hydrochloride)
GNE-617 hydrochloride
2070014-99-05mg900元
2024/04/30HY-15766AGNE-617 (hydrochloride)
GNE-617 hydrochloride
2070014-99-010mM * 1mLin DMSO920元

常见问题列表

生物活性
GNE-617 hydrochloride 是一种特异性的 NAMPT 抑制剂,抑制 NAMPT 活性,IC50 为 5 nM。
靶点

IC50: 5 nM (NAMPT)

体外研究

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 IC 50 values below 100 nM, with approximately half with IC 50 values less than 10 nM. Eighteen cell lines are not rescued with nicotinic acid, and these non-rescuable cell lines tended to have lower IC 50 values (P=0.008, Fisher exact test, IC 50 <10 nM vs. ≥10 nM).

体内研究

In rats, GNE-617 hydrochloride (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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