GNE-618

小分子

GNE-618

G649309-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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. Form:Solid IC50& Target:IC50: 6 nM (NAMPT)

GNE-618 是一种强效的口服活性烟酰胺磷酸核糖转移酶 (NAMPT) 抑制剂，IC50 为 6 nM。GNE-618 可消耗 NAD 水平并诱导肿瘤细胞死亡。抗肿瘤活性。

1362151-42-5

C21H15F3N4O3S

460.43 g/mol

O=C(NCC1=CC=C(S(=O)(C2=CC(C(F)(F)F)=CC=C2)=O)C=C1)C3=CC(C=NN4)=C4N=C3

DMSO : 125 mg/mL (271.49 mM; Need ultrasonic)