| Identification | Back Directory | [Name]
N-(4-((3-(trifluoromethyl)phenyl)sulfonyl)benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide | [CAS]
1362151-42-5 | [Synonyms]
GNE-618
N-(4-((3-(trifluoromethyl)phenyl)sulfonyl)benzyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
1H-Pyrazolo[3,4-b]pyridine-5-carboxamide, N-[[4-[[3-(trifluoromethyl)phenyl]sulfonyl]phenyl]methyl]- | [Molecular Formula]
C21H15F3N4O3S | [MDL Number]
MFCD28411709 | [MOL File]
1362151-42-5.mol | [Molecular Weight]
460.429 |
| Chemical Properties | Back Directory | [Boiling point ]
740.6±60.0 °C(Predicted) | [density ]
1.479±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Soluble | [form ]
Solid | [pka]
8.97±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
GNE-618 is an inhibitor of nicotinamide phosphoribosyl transferase (NAMPT). | [Uses]
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity[1]. | [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[1]. | [References]
[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. DOI:10.1593/neo.131304 |
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