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GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $77 | In Stock | |
10 mg | $126 | In Stock | |
25 mg | $230 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $549 | In Stock | |
500 mg | $1,190 | In Stock | |
1 mL x 10 mM (in DMSO) | $78 | In Stock |
Description | GNE-617, a specific NAMPT inhibitor(IC50=5 nM), shows potency in xenograft models of cancer. |
Targets&IC50 | NAMPT:5 nM |
In vitro | In A549 cell, GNE-617 inhibits NAMPT (IC50=18.9 nM) . |
In vivo | In rat studies, GNE-617 hydrochloride (QD) and GNE-875 (BID) demonstrated greater retinal toxicity at comparable exposures and durations of dosing than did GMX-1778 (BID). The efficacy studies in mice, which evaluated GNE-617, GNE-618, and GMX-1778, also opportunistically investigated retinal toxicity. NAMPTi-induced retinal toxicity was identified in cases involving GNE-617 and GMX-1778. However, varying study durations for GNE-617 and GMX-1778 preclude a direct comparison of their retinal toxicity profiles. |
Kinase Assay | For RNA interference (RNAi), A549 cells are plated at 1,500 cells per well in 96-well plates, allowed to adhere for 24 hours, and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1, 1 , 10 , 100 , and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression, RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin |
Cell Research | GNE-617 is dissolved in DMSO and stored, and then diluted with appropriate media before use.Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC50 values and nicotinic acid rescue status, cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition, the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC50 values are calculated using XLfit 5.1. To examine the protein level, cells are lysed in ice-cold radioimmunoprecipitation assay buffer, run on SDS-PAGE (4%-12% Bis-Tris), and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin |
Animal Research | Male na?ve Sprague Dawley rats are administered once daily via oral gavage with GNE-617( 30?mg/kg), formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) . |
Alias | GNE617 |
Molecular Weight | 427.42 |
Formula | C21H15F2N3O3S |
Cas No. | 1362154-70-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (58.49 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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