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TVB-3664 (TVB3664 ) is a novel and potent fatty acid synthase (FASN) inhibitor that is orally bioavailable, reversible, and selective. It inhibits FASN 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.
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| ln Vitro |
In the CaCo2, HT29, and LIM2405 cell lines, TVB-3664 (0-1 μM, 7 days) demonstrates anti-tumor action [1]. The viability of several tumor cell lines from hematological and solid malignancies is decreased by TVB-3664 [1].
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| ln Vivo |
Tumor volume and weight significantly decreased after 4 weeks of oral gavage treatment with TVB-3664 (3 mg/kg for Pt 2614 and Pt 2449PT) or 6 mg/kg for Pt 2402 and Pt 2449LM). For the Pt 2614 PDX model, the average tumor weight decreased by 30%, 37.5%, and 51.5%, respectively [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: CaCo2, HT29 and LIM2405 cell lines. Tested Concentrations: 0-1 μM. Incubation Duration: 7 days. Experimental Results: demonstrated anti-tumor activity. |
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| Animal Protocol |
Animal/Disease Models: 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].
Doses: 3 mg/kg (Pt 2614 and Pt 2449PT) or 6 mg/kg (Pt 2402 and Pt 2449LM). Route of Administration: po (oral gavage) daily for 4 weeks. Experimental Results: 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. |
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| 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. |
| Molecular Formula |
C25H23F3N4O2
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| Molecular Weight |
468.48
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| Exact Mass |
468.1773
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| CAS # |
2097262-58-1
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| SMILES |
FC(C1=NC(=C(C([H])([H])OC([H])([H])[H])N1[H])C1C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C(C=1[H])C(N1C([H])([H])C([H])(C2C([H])=C([H])C(C#N)=C([H])C=2[H])C1([H])[H])=O)(F)F
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| Synonyms |
TVB3664 TVB 3664 TVB-3664
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~21.35 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1346 mL | 10.6728 mL | 21.3456 mL | |
| 5 mM | 0.4269 mL | 2.1346 mL | 4.2691 mL | |
| 10 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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