Home > Products > Featured products

TVB-3664

  Cat. No.:  DC39632   Featured
Chemical Structure
2097262-58-1
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
TVB-3664 is a FASN inhibitor which significantly reduces tubulin palmitoylation and mRNA expression.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2097262-58-1
Chemical Name: 4-[1-[5-[5-(Methoxymethyl)-2-(trifluoromethyl)-1H-imidazol-4-yl]-2,4-dimethylbenzoyl]azetidin-3-yl]benzonitrile
Synonyms: TVB-3664; TVB 3664; TVB3664
SMILES: FC(C1=NC(=C(COC)N1)C1C(C)=CC(C)=C(C=1)C(N1CC(C2C=CC(C#N)=CC=2)C1)=O)(F)F
Formula: C25H23F3N4O2
M.Wt: 468.470936059952
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DM
Publication: 1: Heuer TS, Ventura R, Mordec K, Lai J, Fridlib M, Buckley D, Kemble G. 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. doi: 10.1016/j.ebiom.2016.12.012. Epub 2016 Dec 24. PubMed PMID: 28159572.
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].
Target: FASN[1][2].
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.
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.
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
DC58047 DSPE-PEG 2000 PEG2000-DSPE is used for creating micelles that are able to carry drugs with low solubility.
DC31000 LP-01 LP-01 is an ionizable cationic amino lipid (pKa = ~6.1). It has been used in the generation of lipid nanoparticles (LNPs). LNPs containing LP-01 and encapsulating both Cas9 mRNA and modified single-guide RNA (sgRNA) for the transport protein transthyretin (Ttr) induce gene editing in liver cells in mice in a dose-dependent manner resulting in reduced serum Ttr levels for at least 12 months.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC66114 FAPI-46 FAPI46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI 46 can be used for tumor imaging of a multitude of different cancers.
DC60580 Endosidin5(ES5) Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC60559 PT-179 PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.
DC65841 MC1 MC1 is a selective and potent inhibitor for COX-2, and [11C]MC1 detected COX-2 in nonhuman primates after intracerebral injection of an inflammogen.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia