A potent Nampt inhibitor
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GNE-617

Item No. 22463

Technical Information
Formal Name
N-[[4-[(3,5-difluorophenyl)sulfonyl]phenyl]methyl]-imidazo[1,2-a]pyridine-6-carboxamide
CAS Number
1362154-70-8
Molecular Formula
C21H15F2N3O3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml
λmax
238 nm
SMILES
FC1=CC(S(C2=CC=C(CNC(C(C=C3)=CN4C3=NC=C4)=O)C=C2)(=O)=O)=CC(F)=C1
InChi Code
InChI=1S/C21H15F2N3O3S/c22-16-9-17(23)11-19(10-16)30(28,29)18-4-1-14(2-5-18)12-25-21(27)15-3-6-20-24-7-8-26(20)13-15/h1-11,13H,12H2,(H,25,27)
InChi Key
XRDVXQQZLHVEQZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GNE-617 is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt; IC50 = 5 nM).1 It has antiproliferative activity in U251 glioblastoma, HT-1080 fibrosarcoma, PC3 prostate, MiaPaCa2 pancreatic, and HCT116 colon cancer cell lines (IC50s = 1.8, 2.1, 2.7, 7.4, and 2.0 nM, respectively). In a U251 mouse xenograft model, GNE-617 (25 mg/kg once per day) led to rapid tumor regression.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zheng, X., Bauer, P., Baumeister, T., et alStructure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors. J. Med. Chem. 56(16), 6413-6433 (2013).