VT103
Based on 5 publication(s) in Google Scholar
VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.64%
- No. CAS: 2290608-13-6
- Fòrmula: C18H17F3N4O2S
- Peso molecular:410.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) VT103
MoreVer todos los productos específicos de isoformas YAP
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Actividad biológica
TEAD1 Palmitoylation[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H2052 | IC50 |
7.13 nM
Compound: 29; VT103
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Anti-proliferative activity against human NCI-H2052 expressing NF2 mutant assessed as cell growth inhibition by CellTiter-Glo Luminescent Cell Viability Assay
Anti-proliferative activity against human NCI-H2052 expressing NF2 mutant assessed as cell growth inhibition by CellTiter-Glo Luminescent Cell Viability Assay
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[PMID: 36063664] |
| NCI-H226 | IC50 |
0.003 μM
Compound: VT-103
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Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
Cytotoxicity against human NCI-H226 cells assessed as cell viability at 10 uM measured for 7 days by celltiter-glo assay
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[PMID: 35763499] |
| NCI-H226 | IC50 |
3.8 nM
Compound: 29; VT103
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Anti-proliferative activity against human NCI-H226 expressing NF2 mutant assessed as cell growth inhibition by CellTiter-Glo Luminescent Cell Viability Assay
Anti-proliferative activity against human NCI-H226 expressing NF2 mutant assessed as cell growth inhibition by CellTiter-Glo Luminescent Cell Viability Assay
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[PMID: 36063664] |
VT103 (HEK293T cells; 3 μM) appeares to be TEAD1-selective, as it does not block palmitoylation of TEAD2, TEAD3, or TEAD4. VT103 (NF2-deficient NCI-H226 cells; 3 mmol/L; 4 or 24 hours) selectively disrupts YAP–TEAD1 interaction[1].
VT103 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1[1].
VT103 shows an IC50 of 1.02 nM in YAP reporter assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetics of VT103 in mice[1]
| Dose | IV | PO | |||||||
| 7 mg/kg | T1/2 (hours) | Vdss (L/kg) | CI(mL/min/kg) | AUC 0-24 hours (μg*h/mL) | AUC 0-24 hours (μg*h/mL) | Oral availability (%) | Cmax (ng/mL) | C24 hours (ng/mL) | |
| 13.2 | 4.5 | 4.7 | 20.0 | 14.9 | 75 | 896 (1 hour) | 340 | ||
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H226-tumor bearing mice[1]
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Dosage:0.3~10 mg/kg
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Administration:P.o. once per day
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Result:Blocked tumor growth even at 0.3 mg/kg.
Chemical Information
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No. CAS 2290608-13-6
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Appearance Solid
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Peso molecular 410.41
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Fòrmula C18H17F3N4O2S
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Color Off-white to gray
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SMILES
O=S(C1=CC=C(NC2=CC=C(C(F)(F)F)C=C2)C(C3=CN(C)C=N3)=C1)(NC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Med Chem
2022 Jul 14;65(13):9206-9229. PMID: 35763499 -
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Solvente y solubilidad
DMSO : 50 mg/mL (121.83 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)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.4366 mL | 12.1829 mL | 24.3659 mL | 60.9147 mL |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8732 mL | 12.1829 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL | 6.0915 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0610 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2183 mL | 3.0457 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4366 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0305 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5229 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6091 mL |
VT103 Related Classifications
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