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2097262-58-1

2097262-58-1 structure
2097262-58-1 structure
  • Name: TVB-3664
  • Chemical Name: TVB-3664
  • CAS Number: 2097262-58-1
  • Molecular Formula: C25H23F3N4O2
  • Molecular Weight: 468.47
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Fatty Acid Synthase (FAS)
  • Create Date: 2019-06-01 10:06:39
  • Modify Date: 2024-01-13 17:52:44
  • TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression[1][2].

Name TVB-3664
Description TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression[1][2].
Related Catalog
Target

FASN[1][2].

In Vitro TVB-3664 (0-1 μM, 7 days) shows anti-tumor activity in CaCo2, HT29 and LIM2405 cell lines[1]. TVB-3664 decreases viability in multiple tumor cell lines from solid and hematopoietic tumor types[1]. Cell Proliferation Assay[1] Cell Line: CaCo2, HT29 and LIM2405 cell lines. Concentration: 0-1 μM. Incubation Time: 7 days. Result: Showed anti-tumor activity.
In Vivo TVB-3664 (3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM), oral gavage, daily, 4 weeks) treatment leads to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively[1]. Animal Model: Colorectal cancer (CRC) PDX models in NOD-SCID-IL2rg-/- (NSG) mice using specimens collected from patients who had undergone surgery for resection of primary CRC or CRC metastasis[1]. Dosage: 3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM). Administration: Oral gavage daily for 4 weeks. Result: Led to a significant reduction in tumor volume and tumor weight in Pt 2614, Pt 2449PT, and Pt 2402 PDX models, with an average reduction in tumor weight of 30%, 37.5% and 51.5%, respectively.
References

[1]. Zaytseva YY, et al. Preclinical evaluation of novel fatty acid synthase inhibitors in primary colorectal cancer cells and a patient-derived xenograft model of colorectal cancer. Oncotarget. 2018 May 15;9(37):24787-24800.

[2]. Heuer TS, et al. FASN Inhibition and Taxane Treatment Combine to Enhance Anti-tumor Efficacy in Diverse Xenograft Tumor Models through Disruption of Tubulin Palmitoylation and Microtubule Organization and FASN Inhibition-Mediated Effects on Oncogenic Signaling and Gene Expression. EBioMedicine. 2017 Feb;16:51-62.

Density 1.36±0.1 g/cm3(Predicted)
Boiling Point 665.7±55.0 °C(Predicted)
Molecular Formula C25H23F3N4O2
Molecular Weight 468.47
Storage condition 2-8°C