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GNE-618

Catalog No. T15403 CAS 1362151-42-5

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.

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GNE-618, CAS 1362151-42-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM). GNE-618 depletes NAD levels and induces tumor cell death. It has anti-tumor activity.
Targets&IC50	NAMPT:6 nM
In vitro	GNE-618 decreases levels of NAD (EC50: 2.6 nM in the NSCLC cell line Calu-6). GNE-618 also reduces cellular proliferation of Calu-6 cells as determined using two different assay formats, either measuring ATP (EC50: 13.6 nM) or total protein content (SRB assay; EC50: 25.8 nM). GNE-618 (10-30 nM; 72 hours) displays an increase in the sub-2N population and a reduction in the percentage of cells in the G1 and M phases of the cell cycle in Calu-6 cells.
In vivo	In STO#81 patient-derived gastric model, 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.

Molecular Weight	460.43
Formula	C21H15F3N4O3S
CAS No.	1362151-42-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

Related Products

Related compounds with same targets

Nampt activator-1 STF-118804 Nampt-IN-1 KPT9274 GNE-617 (E)-Daporinad CHS-828 GNE-618

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Keywords

GNE-618 1362151-42-5 代谢 NAMPT GNE618 GNE 618 Inhibitor inhibitor inhibit

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