| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Fasnall targets fatty acid synthase (FASN), a multifunctional enzyme that catalyzes the synthesis of long-chain fatty acids from acetyl-CoA and malonyl-CoA. By inhibiting FASN, fasnall reduces de novo lipogenesis, depriving cancer cells of the fatty acids required for membrane synthesis, energy production, and signaling. This mechanism induces apoptosis in cancer cells and inhibits tumor growth. FASN is overexpressed in many cancers, making it an attractive therapeutic target.
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| ln Vitro |
Fasnall has IC50 values in HepG2 cells of 147 and 213 nM, respectively, making it a potent foaming agent and moisture absorber into the entire substrate [1]. Proliferation of HER2+ breast cancer cell system sensing Fasnall (50 μM; 24-120 hours) flow-back cell lines Fasnall (25-100 μM; 24-120 hours) [1].
In vitro, fasnall potently inhibits FASN activity with an IC₅₀ in the nanomolar range. The compound shows selectivity for FASN over other metabolic enzymes. In cancer cell lines, fasnall inhibits cell proliferation, induces apoptosis, and reduces lipid synthesis. The compound's anti-proliferative effects have been characterized in various cancer cell types, including breast, colon, and prostate cancer cells. |
| ln Vivo |
In the MMTV-Neu model of HER2+ breast cancer, Fasnall (15 mg/kg, intraperitoneally, twice weekly; 3 weeks) showed strong anticancer efficacy [1].
In vivo, fasnall has demonstrated anti-tumor activity in mouse xenograft models of cancer. The compound inhibits tumor growth and induces apoptosis in tumor tissues. Fasnall also shows anti-obesity effects in animal models by reducing fat accumulation and improving metabolic parameters. The compound's oral bioavailability supports convenient dosing for preclinical studies. |
| Enzyme Assay |
Non-cellular enzyme assays for fasnall involve assessing its inhibition of FASN activity using purified recombinant FASN enzyme. The enzyme is incubated with acetyl-CoA, malonyl-CoA, and NADPH in the presence of varying concentrations of fasnall. The oxidation of NADPH is monitored spectrophotometrically at 340 nm, and IC₅₀ values are determined from dose-response curves. The compound's binding affinity can be assessed using surface plasmon resonance.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF7, MDA-MB-468, BT474 and SKBR3 Cell Tested Concentrations: 50 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours), 96 hrs (hours), 120 hrs (hours) Experimental Results: Inhibition of invasive cell lines proliferated but demonstrated lower activity in the non-tumorigenic cell line MCF10A. Apoptosis analysis [1] Cell Types: MCF7, MDA-MB-468, BT474 and SKBR3 Cell Tested Concentrations: 25 μM, 50 μM, 75 μM, 100 μM Incubation Duration: 24 h Experimental Results: Induction of caspase-3 and caspase-7 activation. In vitro cellular assays for fasnall involve treating cancer cell lines with the compound and assessing cell viability, proliferation, and lipid synthesis. Cell viability is measured using MTT or CellTiter-Glo® assays. Lipid synthesis is assessed by measuring the incorporation of [¹⁴C]-acetate or [¹⁴C]-glucose into lipids. Apoptosis is assessed by flow cytometry using Annexin V/PI staining or by measuring caspase activity. |
| Animal Protocol |
Animal/Disease Models: Female MMTV-NEU mouse cancer cells bearing HER2+ breast cancer [1]
Doses: 15 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a week; 3-week Experimental Results: tumor volume diminished, MMTV- The median survival of Neu mice was extended to 63 days. In vivo animal experiments with fasnall are conducted in mouse xenograft models of cancer and models of obesity. Tumor-bearing mice are treated with fasnall via oral or intraperitoneal administration, and tumor growth inhibition is monitored. In obesity models, mice are fed a high-fat diet and treated with fasnall, and body weight, fat mass, and metabolic parameters are measured. Pharmacokinetic studies characterize absorption and distribution. |
| ADME/Pharmacokinetics |
Fasnall has a molecular weight of 359.46 and a molecular formula of C₂₂H₂₅N₃O₂. It is a solid at room temperature with a purity of ≥98%. The compound is soluble in DMSO and other organic solvents. It is typically stored at -20°C, protected from light and moisture. Fasnall is orally bioavailable with favorable pharmacokinetic properties for preclinical studies.
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| Toxicity/Toxicokinetics |
Fasnall is a research compound for laboratory use only and is not approved for human therapeutic use. In preclinical studies, it has been generally well-tolerated at therapeutic doses. As a FASN inhibitor, it may have effects on normal tissues that depend on de novo lipogenesis. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation.
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| References | |
| Additional Infomation |
Fasnall is a racemic mixture composed of equimolar amounts of (R)-Fasnall and (S)-Fasnall. Both enantiomers can act as fatty acid synthase inhibitors, but the (S)-enantiomer is more than four times more active than the (R)-enantiomer. It has multiple functions, including as a fatty acid synthesis inhibitor, an EC 2.3.1.85 (fatty acid synthase) inhibitor, an apoptosis inducer, and an anti-HIV drug. It comprises one (R)-Fasnall and one (S)-Fasnall.
Fasnall (CAS 929978-58-5) is a potent and selective inhibitor of fatty acid synthase (FASN), a key enzyme in de novo lipogenesis. It is being investigated for anti-cancer and anti-obesity properties. Fasnall induces apoptosis in cancer cells and inhibits tumor growth in preclinical models. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C25H28N4O3S2
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| Molecular Weight |
496.644823074341
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| Exact Mass |
496.16
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| CAS # |
929978-58-5
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| PubChem CID |
16230362
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| Appearance |
Light yellow to brown solid powder
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| LogP |
4.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
414
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(SC2=NC=NC(=C12)NC3CCN(C3)CC4=CC=CC=C4)C
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| InChi Key |
VSXRMURGJRAOCU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N4S/c1-13-14(2)24-19-17(13)18(20-12-21-19)22-16-8-9-23(11-16)10-15-6-4-3-5-7-15/h3-7,12,16H,8-11H2,1-2H3,(H,20,21,22)
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| Chemical Name |
N-(1-benzylpyrrolidin-3-yl)-5,6-dimethylthieno[2,3-d]pyrimidin-4-amine
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0135 mL | 10.0677 mL | 20.1353 mL | |
| 5 mM | 0.4027 mL | 2.0135 mL | 4.0271 mL | |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0135 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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