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GNE-618

Chemical Structure : GNE-618

CAS No.: 1362151-42-5

GNE-618 (GNE618)

Catalog No.: PC-38787Not For Human Use, Lab Use Only.

GNE-618 is a potent, selective NAMPT inhibitor with IC50 of 6 nM, depletes NAD and induces cell death in vitro and in vivo.

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Biological Activity

GNE-618 is a potent, selective NAMPT inhibitor with IC50 of 6 nM, depletes NAD and induces cell death in vitro and in vivo.
GNE-618 reduced levels of NAD with an 50% minimal response (EC50) of 2.6 nM in the NSCLC cell line Calu-6, reduced cellular proliferation of Calu-6 cells with IC50 of 13. 6 nM.
NAMPT, but not NAPRT1, mRNA and protein levels inversely correlate with sensitivity to GNE-618 across a panel of 53 non-small cell lung carcinoma cell lines.
GNE-618 inhibits in vivo tumor growth in an A549 non-small cell lung carcinoma (NSCLC) model.

Physicochemical Properties

M.Wt 460.43
Formula C21H15F3N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[[4-[[3-(Trifluoromethyl)phenyl]sulfonyl]phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide

References

1. O'Brien T, et al. Neoplasia. 2013 Dec;15(12):1314-29.

2. Xiao Y, et al. Neoplasia. 2013 Oct;15(10):1151-60.

3. Zheng X, et al. J Med Chem 2013;56:6413–33.

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