VT103 |
Katalog-Nr.GC63257
One-Click Copy Product Info
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VT103, ein Analogon von VT101, ist ein oral aktiver und selektiver Palmitoylierungsinhibitor des TEAD1-Proteins. VT103 hemmt die durch YAP/TAZ-TEAD gefÖrderte Gentranskription, blockiert die TEAD-Autopalmitoylierung und unterbricht die Wechselwirkung zwischen YAP/TAZ und TEAD. VT103 kann fÜr die Krebsforschung eingesetzt werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2290608-13-6
Sample solution is provided at 25 µL, 10mM.
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VT103 is a selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD-mediated gene transcription, blocks TEAD auto-palmitoylation, and disrupts the interaction between YAP/TAZ and TEAD[1-2]. VT103 can be used in research related to HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer[3-4].
In vitro, VT103 (10μM) was used to treat neonatal mouse cardiac fibroblasts (NMCFs) stimulated with angiotensin II (Ang-II; 100nM) for 48 hours. VT103 reversed the Ang-II-induced increase in α-SMA expression and inhibited collagen gel contraction and cell migration[5]. VT103 (10μM) was also used to treat human coronary artery smooth muscle cells (HCASMCs) overexpressing METTL14 for 24 hours. VT103 inhibited the expression of TEAD1, PDGFRB, CTGF, and Cyr61, restored the expression of contractile markers ACTA2, CNN1, and SM22α, and attenuated the METTL14 overexpression-enhanced cell viability, proliferation, and migration[6].
In vivo, VT103 (100mg/kg) combined with Dabrafenib (30mg/kg) was administered orally daily for 14 days to treat female BALB/c-nu mice bearing KTOR81 xenograft tumors. VT103 significantly inhibited tumor growth and maintained sustained tumor regression during a 42-day observation period, without significantly affecting mouse body weight[7]. VT103 (0.3, 1, 3mg/kg) was administered orally daily for 45 days to treat mice bearing NCI-H226 xenograft tumors. VT103 significantly inhibited tumor growth, and at the 3mg/kg dose, VT103 induced tumor regression without significantly affecting body weight during the treatment period[8].
References:
[1] Heinrich T, Peterson C, Schneider R, et al. Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106. J Med Chem. 2022 Jul 14;65(13):9206-9229.
[2] Vaparanta K, Song Z, Farahani I, et al. Phosphoproteomic analysis reveals the diversity of signaling behind ErbB-inhibitor-induced phenotypes. FEBS J. 2025 Dec;292(24):6557-6575.
[3] Zhang S, Tan YQ, Zhang X, et al. TFF3 drives Hippo dependent EGFR-TKI resistance in lung adenocarcinoma. Oncogene. 2025 Mar;44(11):753-768.
[4] Evsen L, Morris PJ, Thomas CJ, et al. Comparative Assessment and High-Throughput Drug-Combination Profiling of TEAD-Palmitoylation Inhibitors in Hippo Pathway Deficient Mesothelioma. Pharmaceuticals (Basel). 2023 Nov 21;16(12):1635.
[5] Song S, Zhang X, Huang Z, et al. TEA domain transcription factor 1(TEAD1) induces cardiac fibroblasts cells remodeling through BRD4/Wnt4 pathway. Signal Transduct Target Ther. 2024 Feb 19;9(1):45.
[6] Wang L, Xia G, Tang Y, et al. METTL14 Promotes Vascular Smooth Muscle Cell Proliferation and Neointima Formation via m6A Methylation TEAD1 mRNA. J Biochem Mol Toxicol. 2025 May;39(5):e70284.
[7] Hosoya K, Ozasa H, Yoshida H, et al. Novel TEAD1 Inhibitor VT103 Enhances Dabrafenib Efficacy in BRAF V600E Mutated Lung Adenocarcinoma via Survivin Downregulation. Cancer Sci. 2025 Jul;116(7):1883-1896.
[8] Tang TT, Konradi AW, Feng Y, et al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021 Jun;20(6):986-998.
| Cell experiment [1]: | |
Cell lines | Neonatal Mice Cardiac Fibroblasts (NMCFs) |
Preparation Method | Neonatal Mice Cardiac Fibroblasts (NMCFs) were stimulated with angiotensin II (Ang-II; 100nM). The cells were treated with VT103 (10μM) for 48 hours. |
Reaction Conditions | 10μM; 48h. |
Applications | VT103 reversed the Ang-II-induced increase in α-SMA expression. VT103 also inhibited collagen gel contraction and cell migration. |
| Animal experiment [2]: | |
Animal models | Six-week-old female BALB/c-nu mice |
Preparation Method | KTOR81 cells (5x10⁶) suspended in Matrigel were injected subcutaneously into the backs of the mice. Treatment was initiated when the tumor volume reached 200mm³. The mice was treated with VT103 (100mg/kg). |
Dosage form | 100mg/kg; p.o.; daily administration for 14 days. |
Applications | The combination of Dabrafenib and VT103 induced significant tumor shrinkage and showed a sustained response with maintained tumor regression during the 42 days observation period. The combination therapy did not cause significant adverse effects on the body weight of the mice. |
References: | |
| Cas No. | 2290608-13-6 | SDF | |
| Formula | C18H17F3N4O2S | M.Wt | 410.41 |
| Löslichkeit | DMSO : 50 mg/mL (121.83 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4366 mL | 12.1829 mL | 24.3659 mL |
| 5 mM | 487.3 μL | 2.4366 mL | 4.8732 mL |
| 10 mM | 243.7 μL | 1.2183 mL | 2.4366 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)