GNE-618 是一种有效的，具有口服活性的烟酰胺磷酸核糖基转移酶 (NAMPT) 抑制剂，IC₅₀ 为 6 nM。GNE-618 消耗 NAD 水平并诱导细胞死亡，具有抗肿瘤活性。

GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC 50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.

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IC50: 6 nM (NAMPT)

GNE-618 reduces levels of NAD with an EC50 of 2.6 nM in the NSCLC cell line Calu-6.
GNE-618 (10-30 nM; 72 hours) reveals an increase in the sub-2N population and a decreases in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells.
GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50 of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC50 of 25.8 ± 4.2 nM) has not independently confirmed the accuracy of these methods. They are for reference only.

GNE-618 (100 mg/kg; p.o.; twice daily for 5 days) significantly inhibits tumor growth by 88% and has minimal effects on body weight in STO#81 patient-derived gastric model. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Xiao Y, et al. Dependence of tumor cell lines and patient-derived tumors on the NAD salvage pathway rendersthem sensitive to NAMPT inhibition with GNE-618. Neoplasia. 2013 Oct;15(10):1151-60.

In Vitro: DMSO : 125 mg/mL (271.49 mM; Need ultrasonic)配制储备液