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Key Documents

SML1694

Sigma-Aldrich

TVB-3166

≥98% (HPLC)

Synonym(s):

4-(1-(5-(3,4-Dimethyl-1H-pyrazol-5-yl)-2,4-dimethylbenzoyl)azetidin-3-yl)benzonitrile

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About This Item

Empirical Formula (Hill Notation):
C24H24N4O
CAS Number:
Molecular Weight:
384.47
UNSPSC Code:
41106300
PubChem Substance ID:
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

protect from light

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

CC1=C(C2=C(C)C(C)=NN2)C=C(C(N3CC(C4=CC=C(C#N)C=C4)C3)=O)C(C)=C1

Biochem/physiol Actions

TVB-3166 is a cell-permeable pyrrazole derivative that inhibits cellular palmitate synthesis (IC50 <100 nM) by fatty acid synthase (FASN) keto-reductase activity in a potent and reversible manner (IC50 = 42 nM), effectively inhibiting palmitate-dependent survival of various cancer cells in cultures and xenografted tumor growth in mice vivo (60-100 mg/kg/d p.o.), while exhibiting little or no anti-proliferation activity toward non-palmitate-dependent growth of cancer and non-cancer cultures. FASN inhibition by TVB-3166 treatment is also effective against the replications respiratory viruses both in cultures (Effc. conc. 200 nM against RSV and PIV3 in A549, HEp2, and HeLa cultures) and in mice (50 mg/kg/12 h, p.o.; RSV) in vivo without significant adverse effects to the host cells or mice.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Barbara Schroeder et al.
Cell death & disease, 12(11), 977-977 (2021-10-23)
Inhibitors of the lipogenic enzyme fatty acid synthase (FASN) have attracted much attention in the last decade as potential targeted cancer therapies. However, little is known about the molecular determinants of cancer cell sensitivity to FASN inhibitors (FASNis), which is
Jiajun Du et al.
Nature communications, 11(1), 4830-4830 (2020-09-26)
Non-invasively probing metabolites within single live cells is highly desired but challenging. Here we utilize Raman spectro-microscopy for spatial mapping of metabolites within single cells, with the specific goal of identifying druggable metabolic susceptibilities from a series of patient-derived melanoma

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