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Chemical Structure| 1399177-37-7 Chemical Structure| 1399177-37-7

Structure of Denifanstat
CAS No.: 1399177-37-7

Chemical Structure| 1399177-37-7

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Denifanstat is an orally effective FASN inhibitor that inhibits fatty acid synthesis, showing significant application potential in research on fatty liver and cancer.

Synonyms: TVB-2640; FASN-IN-2; Fatty Acid Synthase Inhibitor 2, FASN-IN-2

4.5 *For Research Use Only !

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Product Details of Denifanstat

CAS No. :1399177-37-7
Formula : C27H29N5O
M.W : 439.55
SMILES Code : N#CC1=CC=C(C2CCN(C(C3=CC(C4=NC(C)=NN4)=C(C5CCC5)C=C3C)=O)CC2)C=C1
Synonyms :
TVB-2640; FASN-IN-2; Fatty Acid Synthase Inhibitor 2, FASN-IN-2
MDL No. :MFCD32197184

Safety of Denifanstat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A375M6, SkMel28, SkMel2 melanoma cells 10 μM 24 hours To evaluate the effect of Denifanstat on cell survival and colony formation ability in suspension, results showed that Denifanstat had no significant effect on cell survival and colony formation ability PMC11338773
PANC-1 cells 10 nmol/L 48 hours To evaluate the synergistic effect of TVB-3166 with BH3 mimetics (ABT-263/navitoclax and ABT-199/venetoclax), results showed that TVB-3166 significantly enhanced the apoptotic cell death induced by BH3 mimetics. PMC11908614
MIA PaCa-2 cells 10 nmol/L 48 hours To evaluate the synergistic effect of TVB-3166 with BH3 mimetics (ABT-263/navitoclax and ABT-199/venetoclax), results showed that TVB-3166 significantly enhanced the apoptotic cell death induced by BH3 mimetics. PMC11908614
BxPC-3 cells 10 nmol/L 48 hours To evaluate the synergistic effect of TVB-3166 with BH3 mimetics (ABT-263/navitoclax and ABT-199/venetoclax), results showed that BxPC-3 cells were insensitive to the synergistic effect of TVB-3166 with BH3 mimetics. PMC11908614
Human primary liver microtissues 30 nM and 3 µM 10 days Reduced triglyceride content, showing direct anti-steatotic activity PMC9485253
Human hepatic stellate cells 150 nM 48 hours Reduced markers of fibrosis, including collagen1α1 and α-smooth muscle actin PMC9485253
CD4+ T cells 50 nM and 100 nM Reduced production of Th17 cells and increased regulatory T cells PMC9485253
Huh7 cells 10 μM 16 hours To investigate the effect of TOFA on MERS-CoV replication, results showed that TOFA treatment significantly reduced the release of infectious viral progeny PMC11915874
MRC5 cells 10 μM 16 hours To investigate the effect of TOFA on MERS-CoV replication, results showed that TOFA treatment significantly reduced the release of infectious viral progeny PMC11915874
HEK293T-hACE2 5 µM 16 h Screening FAS inhibitors for their ability to inhibit SARS-CoV-2 infection, 11 FAS inhibitors were found to significantly inhibit viral replication. PMC8475461
MDA-MB-231-BR 1 μM 5 days To test the effect of TVB-2640 on cell migration and invasion, results showed that TVB-2640 significantly slowed down cell migration and invasion. PMC11164988
MDA-MB-231 1 μM 5 days To test the effect of TVB-2640 on cell migration and invasion, results showed that TVB-2640 significantly slowed down cell migration and invasion. PMC11164988
PDO-BC25 1 μM 5 days To test the effect of TVB-2640 on cell migration and invasion, results showed that TVB-2640 significantly slowed down cell migration and invasion. PMC11164988
PDO-BC25-2 1 μM 5 days To test the effect of TVB-2640 on cell migration and invasion, results showed that TVB-2640 significantly slowed down cell migration and invasion. PMC11164988
PL-45 1 μM, 5 μM, 10 μM, 25 μM, 50 μM 24 h, 48 h, 72 h To test the effect of TVB-2640 on the proliferation of PL-45 cells, results showed no significant activity in PDAC cells PMC9847120
SW1990 1 μM, 5 μM, 10 μM, 25 μM, 50 μM 24 h, 48 h, 72 h To test the effect of TVB-2640 on the proliferation of SW1990 cells, results showed no significant activity in PDAC cells PMC9847120
LNCaP 1 μM, 5 μM, 10 μM, 25 μM, 50 μM 24 h, 48 h, 72 h To test the effect of TVB-2640 on the proliferation of LNCaP cells, results showed a significant reduction in proliferation in PCa cells PMC9847120
C4-2 1 μM, 5 μM, 10 μM, 25 μM, 50 μM 24 h, 48 h, 72 h To test the effect of TVB-2640 on the proliferation of C4-2 cells, results showed a significant reduction in proliferation in PCa cells PMC9847120

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Foxn1nu/Foxn1nu athymic mice PANC-1 xenograft model Oral gavage 2% 4 weeks To evaluate the synergistic antitumor effect of TVB-3166 with BH3 mimetics (ABT-263/navitoclax and ABT-199/venetoclax) in vivo, results showed that the combination of TVB-3166 with BH3 mimetics significantly inhibited the growth of PANC-1 xenograft tumors. PMC11908614
Mice Diet-induced NASH models Oral 500 mg/kg/day Once daily, continued until the end of the experiment Prevented development of hepatic steatosis and fibrosis, and reduced circulating IL-1β PMC9485253
Mouse K18-hACE2 transgenic mice Intraperitoneal injection 2.5 mg/kg Every other day, starting from 1 week after model construction Evaluating the efficacy of Orlistat in SARS-CoV-2-infected mice, results showed that Orlistat significantly prolonged survival and reduced viral replication in the lungs. PMC8475461

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03808558 KRAS Gene Mutation PHASE2 ACTIVE_NOT_RECRUITING 2026-12-01 University of Cincinnati, Cinc... More >>innati, Ohio, 45267, United States|University of Texas Southwestern Medical Center, Dallas, Texas, 75390-9179, United States Less <<
NCT02223247 Solid Malignant Tumor PHASE1 COMPLETED 2025-06-17 Scottsdale, Arizona, 85258, Un... More >>ited States|Denver, Colorado, 80218, United States|Sarasota, Florida, 34232, United States|Oklahoma City, Oklahoma, 73104, United States|Nashville, Tennessee, 37203, United States|Dallas, Texas, 75390, United States|San Antonio, Texas, 78229, United States|Charthouse Square, London, United Kingdom|London, W1G 6AD, United Kingdom|Manchester, United Kingdom|West Smithfield, London, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.38mL

2.28mL

1.14mL

22.75mL

4.55mL

2.28mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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