Size : 5mg
Synonyms: TVB-2640, TVB2640, FASN-IN-2
| Description | Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis. |
| Targets & IC50 | FASN:0.072 μM (EC50), FASN:0.052 μM |
| In vitro | METHODS: MDA-MD-231 and MDA-MB-231-BR cells were treated with Denifanstat (1-10.3 µM) for 6-30 h. Cell migration was detected by wound healing assay. RESULTS: Cell migration was inhibited in MDA-MB-231-BR cells but not in parental MDA-MD-231 cells in a dose-dependent manner. [1] |
| In vivo | METHODS: To assay antitumor activity in vivo, Denifanstat (100 mg/kg, 30% PEG400) was administered by gavage to SCID mice bearing PC-3M/HOXB13KD xenografts once daily for six weeks. RESULTS: Five weeks after inoculation, HOXB13-KD mice showed significant metastasis in IVIS, which was completely alleviated by Denifanstat treatment.Denifanstat treatment significantly prolonged metastasis-free survival in both control and HOXB13-KD mice. [2] |
| Synonyms | TVB-2640, TVB2640, FASN-IN-2 |
| Molecular Weight | 439.55 |
| Formula | C27H29N5O |
| Cas No. | 1399177-37-7 |
| Smiles | Cc1n[nH]c(n1)-c1cc(C(=O)N2CCC(CC2)c2ccc(cc2)C#N)c(C)cc1C1CCC1 |
| Relative Density. | 1.27 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 262.5 mg/mL (597.2 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 10 mg/mL (22.75 mM), Solution. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (13.65 mM), Solution. 10% DMSO+40% PEG300+ 5% Tween 80 + 45% Saline: 6 mg/mL (13.65 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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