A FASN inhibitor
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TVB-3166

Item No. 33533

Technical Information
Formal Name
4-[1-[5-(4,5-dimethyl-1H-pyrazol-3-yl)-2,4-dimethylbenzoyl]-3-azetidinyl]-benzonitrile
CAS Number
1533438-83-3
Molecular Formula
C24H24N4O
Formula Weight
Purity
≥98%
A solid
λmax
234 nm
SMILES
N#CC1=CC=C(C2CN(C2)C(C3=CC(C4=NNC(C)=C4C)=C(C)C=C3C)=O)C=C1
InChi Code
InChI=1S/C24H24N4O/c1-14-9-15(2)22(10-21(14)23-16(3)17(4)26-27-23)24(29)28-12-20(13-28)19-7-5-18(11-25)6-8-19/h5-10,20H,12-13H2,1-4H3,(H,26,27)
InChi Key
ICDQFUFDAFKCAX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TVB-3166 is an inhibitor of fatty acid synthase (FASN; IC50 = 0.042 µM).1 It inhibits the biosynthesis of palmitate (Item No. 10010279) in Calu-6 non-small cell lung cancer (NSCLC) cells and MRC-5 lung fibroblasts in a concentration-dependent manner. TVB-3166 (0.2 µM) induces apoptosis in Calu-6, as well as 22Rv1 prostate cancer, cells. It reduces tumor growth in an OVCAR-8 mouse xenograft model and K-Ras-wild-type or -mutant patient-derived xenograft (PDX) mouse models when administered at a dose of 60 mg/kg. TVB-3166 (50 mg/kg) also reduces lung viral titers in mice infected with respiratory syncytial virus A (RSV-A).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ventura, R., Mordec, K., Waszczuk, J., et alInhibition of de novo palmitate synthesis by fatty acid synthase induces apoptosis in tumor cells by remodeling cell membranes, inhibiting signaling pathways, and reprogramming gene expression. EBioMedicine 2(8), 808-824 (2015).

    2. Ohol, Y.M., Wang, Z., Kemble, G., et alDirect inhibition of cellular fatty acid synthase impairs replication of respiratory syncytial virus and other respiratory viruses. PLoS One 10(12), e0144648 (2015).