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 In Vitro GNE-618 reduces levels of NAD with an EC 50 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 (EC 50 of 13.6 ± 1.8 nM) or total protein content (SRB assay; EC 50 of 25.8 ± 4.2 nM)MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 6 nM (NAMPT)
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GNE-618
CAS number：1362151-42-5(DMSO) molecular formula：C21H15F3N4O3S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1362151-42-5(DMSO) | molecular formula | C21H15F3N4O3S |
| molecular weight | 460.43 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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