TVB-3166
Based on 12 publication(s) in Google Scholar
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.69%
- CAS No.: 1533438-83-3
- 화학식: C24H24N4O
- 분자량:384.47
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- Protocol
- 순도&문서
- References
-
Help & FAQs
-
HY-112829
DenifanstatFASN Inhibitor -
HY-B0218
OrlistatFASN Inhibitor -
HY-120062
TVB-3664FASN Inhibitor -
HY-12364
C75Fatty Acid Synthase Inhibitor -
HY-A0210
CeruleninFASN Inhibitor -
HY-121250
FasnallFASN Inhibitor -
HY-111551
FT113FASN Inhibitor -
HY-12325
GSK2194069FASN Inhibitor -
HY-N2486
DesoxyrhaponticinFASN Inhibitor -
HY-16450
SB 204990ATP Citrate Lyase Inhibitor -
HY-14452
FatostatinSREBP Activation Inhibitor -
HY-B0218R
Orlistat (Standard)
Publications Citing Use of MedChemExpress (MCE) TVB-3166
More- Nat Metab. 2021 Nov;3(11):1466-1475. [Abstract]
- Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]
- J Immunother Cancer. 2025 Apr 12;13(4):e010924. [Abstract]
- J Transl Med. 2024 Jan 13;22(1):55. [Abstract]
- Br J Cancer. 2023 Mar;128(7):1344-1359. [Abstract]
- Neurosci Bull. 2025 Jun 28. [Abstract]
- EMBO Rep. 2023 Dec 6;24(12):e49561. [Abstract]
- ACS Omega. 2024 Feb 28;9(10):11870-11882. [Abstract]
- J Cell Sci. 2025 May 15;138(10):jcs263688. [Abstract]
- Biomed Pharmacother. 2025 Nov:192:118656. [Abstract]
- University of Rijeka. 2023.
- McGill University. 2021 Aug, 30347448.
Customer Validation & Images
-
WB
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
2D/3D Cell Culture and Differentiation
-
ELISA
Biological Activity
제품 설명
IC50 & Target
IC50: 42 nM (FASN) and 81 nM (cellular palmitate synthesis)[1]
In Vitro
ISX-9 promotes neurogenesis in vivo, enhancing the proliferation and differentiation of hippocampal subgranular zone (SGZ) neuroblasts, and the dendritic arborization of adult-generated dentate gyrus neurons. At 2.5-20 μM, ISX-9 has been shown to dose-dependently trigger neurogenesis and block gliogenesis in adult rat hippocampal stem cells through a calcium-activated signaling pathway dependent on myocyte-enhancer factor 2-dependent gene expression[1].
Molecular exploration of ISX-9-induced regulation of neurogenesis (via FACS and microarray of SGZ stem and progenitor cells) suggested the involvement of the myocyte-enhancer family of proteins (Mef2)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:CALU-6 tumor cells
-
Concentration:0.001, 0.01, 0.1, 1, 10 μM
-
Incubation Time:24 hours
-
Result:Caused cell death in CALU-6 non-small-cell lung tumor cells with a cellular IC50 value of 0.10 μM.
-
Cell Line:90 different tumor cell lines (such as CALU-6 NSCLC cell line, NCI-H1975 NSCLC cell line)
-
Concentration:0.02 or 0.20 μM
-
Incubation Time:7 days
-
Result:Dose-dependent induction of cell death was observed in all tumor cell lines.
-
Cell Line:COLO-205 and A549 cells
-
Concentration:0.2 μM
-
Incubation Time:48 hours
-
Result:Inhibited β-catenin pathway signal transduction and transcriptional activity.
In Vivo
TVB-3166 (Oral gavage; 30-100 mg/kg/day) has the concentration is approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB-c-nude mice[1]
-
Dosage:30, 60, or 100 mg/kg
-
Administration:Oral gavage; once daily
-
Result:Inhibited xenograft tumor growth.
-
Animal Model:Female BALB-c-nude mice[1]
-
Dosage:30, 60, or 100 mg/kg (Pharmacokinetic Study)
-
Administration:Oral gavage; once daily
-
Result:The concentration was approximately 3-fold higher in plasma than tumor. The 100 and 30 mg/kg groups had plasma and tumor concentrations of 7 and 2.9 μM, respectively.
Chemical Information
-
CAS No. 1533438-83-3
-
Appearance Solid
-
분자량 384.47
-
화학식 C24H24N4O
-
Color White to off-white
-
SMILES
N#CC1=CC=C(C2CN(C(C3=CC(C4=NNC(C)=C4C)=C(C)C=C3C)=O)C2)C=C1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
-
Journal Impact Factor
-
Most Recent
-
Nat Metab
2021 Nov;3(11):1466-1475. PMID: 34580494 -
Nat Commun
Lipogenic enzyme FASN promotes mutant p53 accumulation and gain-of-function through palmitoylation. [Abstract]2025 Feb 19;16(1):1762. PMID: 39971971
TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]
Inhibition of FASN by TVB-3166 reduced the protein levels of mutp53, but not wtp53, in different cells. Cells were treated with the small-molecule FASN inhibitor TVB-3166 (TVB) at the indicated concentrations for 24 h and subjected to Western blot analysis.
TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]
The FASN inhibitor TVB-3166 (TVB, 72 h) displayed a more pronounced inhibitory effect on AIG in cancer cells carrying mutp53 compared with cells with mutp53 KO (a) or knockdown (b). Left in a: Representative images. Scale bar: 200 μm.
TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]
TVB-3166 (TVB) displayed a more pronounced inhibitory effect on the growth of orthotopic tumors formed by SK-BR3 (R175H) cells than tumors formed by SK-BR3 with mutp53 KO. Mice were treated with TVB-3166 (60 mg/kg; i.g.) once every two days for 3 weeks when tumor sizes reached ~30 mm3.
TVB-3166 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 19;16(1):1762. [Abstract]
TVB-3166 (40 μM) treatment displayed a more pronounced inhibitory effect on human colorectal tumor organoids expressing mutp53 compared with organoids expressing wtp53. Left panels: Representative images of different organoids expressing mutp53 or wtp53, which were treated with or without TVB-3166 for 48 h. Scale bar: 50 μm. Right panel: The relative viability of mutp53 and wtp53 organoids.
-
J Immunother Cancer
Targeting B7-H3 inhibition-induced activation of fatty acid synthesis boosts anti-B7-H3 immunotherapy in triple-negative breast cancer. [Abstract]2025 Apr 12;13(4):e010924. PMID: 40221152 -
J Transl Med
Metabolic reprogramming based on RNA sequencing of gemcitabine-resistant cells reveals the FASN gene as a therapeutic for bladder cancer. [Abstract]2024 Jan 13;22(1):55. PMID: 38218866 -
Br J Cancer
Transcriptome analysis of newly established carboplatin-resistant ovarian cancer cell model reveals genes shared by drug resistance and drug-induced EMT. [Abstract]2023 Mar;128(7):1344-1359. PMID: 36717670 -
Neurosci Bull
2025 Jun 28. PMID: 40580390 -
EMBO Rep
2023 Dec 6;24(12):e49561. PMID: 37943703 -
ACS Omega
Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]2024 Feb 28;9(10):11870-11882. PMID: 38496939 -
J Cell Sci
Tumor acidosis supports cancer cell lipid uptake via a rapid transporter-independent mechanism. [Abstract]2025 May 15;138(10):jcs263688. PMID: 40190115 -
Biomed Pharmacother
Modeling of glucocorticoid resistance in multiple myeloma reveals mechanisms and markers of glucocorticoid resistance. [Abstract]2025 Nov:192:118656. PMID: 41138658
TVB-3166 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Nov:192:118656. [Abstract]
Enzyme-linked immunosorbent assay (ELISA) was used to determine the FASN content of xenograft tumors in each group. The ELISA results showed that TVB-3166 (60 mg/kg; i.g.; 5 weeks) reduced the FASN gene of the tumor.
TVB-3166 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2025 Nov:192:118656. [Abstract]
Statistical analysis was performed on the rate of KI67- and TUNEL-positive cells in each group of xenograft tumors by immunohistochemical staining (IHC). The corrected total cell fluorescence (CTCF) of BODIPY staining was used to quantitatively detect the lipid content of xenograft tumors in each group. The results showed that TVB-3166 (60 mg/kg; i.g.; 5 weeks) treatment can reduce lipid accumulation, inhibit cell proliferation and increase the apoptosis rate.
-
-
용액&용해도
In Vitro:
DMSO : 62.5 mg/mL (162.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
-
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
-
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
-
Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
-
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
-
Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
-
Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
-
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
-
Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
-
Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
순도&문서
-
Data Sheet (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6010 mL | 13.0049 mL | 26.0098 mL | 65.0246 mL |
| 5 mM | 0.5202 mL | 2.6010 mL | 5.2020 mL | 13.0049 mL | |
| 10 mM | 0.2601 mL | 1.3005 mL | 2.6010 mL | 6.5025 mL | |
| 15 mM | 0.1734 mL | 0.8670 mL | 1.7340 mL | 4.3350 mL | |
| 20 mM | 0.1300 mL | 0.6502 mL | 1.3005 mL | 3.2512 mL | |
| 25 mM | 0.1040 mL | 0.5202 mL | 1.0404 mL | 2.6010 mL | |
| 30 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | 2.1675 mL | |
| 40 mM | 0.0650 mL | 0.3251 mL | 0.6502 mL | 1.6256 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3005 mL | |
| 60 mM | 0.0433 mL | 0.2167 mL | 0.4335 mL | 1.0837 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3251 mL | 0.8128 mL | |
| 100 mM | 0.0260 mL | 0.1300 mL | 0.2601 mL | 0.6502 mL |
TVB-3166 Related Classifications
HY-120394 Related Classifications
Powered by Bioz