A Nampt inhibitor
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GNE-618

Item No. 37223

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[4-[[3-(trifluoromethyl)phenyl]sulfonyl]phenyl]methyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
CAS Number
1362151-42-5
Molecular Formula
C21H15F3N4O3S
Formula Weight
460.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
227 nm
SMILES
O=C(C1=CC2=C(NN=C2)N=C1)NCC3=CC=C(S(=O)(C4=CC(C(F)(F)F)=CC=C4)=O)C=C3
InChi Code
InChI=1S/C21H15F3N4O3S/c22-21(23,24)16-2-1-3-18(9-16)32(30,31)17-6-4-13(5-7-17)10-26-20(29)15-8-14-12-27-28-19(14)25-11-15/h1-9,11-12H,10H2,(H,26,29)(H,25,27,28)
InChi Key
LKBHAGGICJWHQQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $184

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    10 mg

    $306

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    Cayman Chemical
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    Product Description

    GNE-618 is an inhibitor of nicotinamide phosphoribosyltransferase (Nampt; IC50 = 6.1 nM for the human enzyme).1 It reduces NAD+ levels in PC3 prostate cancer cells (EC50 = 1.2 nM) and inhibits the proliferation of A2780 ovarian cancer cells (IC50 = 4.3 nM). GNE-618 (100 mg/kg) induces tumor regression in an A2780 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zheng, X., Bair, K.W., Bauer, P., et al. Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT). Bioorg. Med. Chem. Lett. 23(20), 5488-5497 (2013).