VT3989
Based on 1 Customer Validation
VT3989 is an orally active pan-TEAD autopalmitoylation inhibitor that modulates the Hippo signaling pathway. VT3989 directly binds to TEAD transcription factors to block their palmitoylation modification, thereby disrupting the formation of YAP/TAZ-TEAD complexes and inhibiting downstream oncogenic transcriptional activity. VT3989 effectively inhibits the growth of NF2-deficient schwannoma and meningioma cells and reverses the Schwann cell phenotype. In addition, VT3989 exerts a synergistic effect when combined with Osimtinib (HY-15772) in EGFR-mutant non-small cell lung cancer models, significantly delaying tumor recurrence and prolonging survival. VT3989 can be used for the research of epithelioid hemangioendothelioma, malignant pleural mesothelioma, type 2 neurofibromatosis and related advanced solid tumors.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 2506273-81-8
- Formula: C21H18F3NO3
- Molecular Weight:389.37
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Differentiation Inducing Compound Library
HY-L038
-
Reprogramming Compound Library
HY-L039
-
Orally Active Compound Library
HY-L061
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Angiogenesis-Related Compound Library
HY-L088
-
Transcription Factor-Targeted Library
HY-L090
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Cytokine Inhibitors Library
HY-L161
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
MCE Bioactive Compound Library
HY-L001V
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
|
YAP/TAZ |
VT3989 exhibits strong to very strong synergy with osimertinib in cell proliferation assays using EGFR mutant NSCLC cell lines[3].
VT3989, a TEAD central pocket inhibitor, reduces expression of TEAD target genes and is cytotoxic to NF2-deficient IOMM-Lee and MG309 meningioma cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Periostin-CRE;NF2fl/fl mice (5-month-old; male and female; age-matched NF2fl/fl-CRE- littermate controls; biallelic NF2/merlin loss in Schwann cells)[2]
-
Dosage:30 mg/kg
-
Administration:p.o.; daily; 21 days
-
Result:Reversed the 2-fold increase in normalized Vegfa expression seen in vehicle-treated NF2fl/fl-Cre+ mice, returning levels to those seen in NF2fl/fl-Cre- control mice.
Reduced Schwann cell-associated Vegfa signal in dorsal root ganglia of treated mice, with no change in neuron-associated Vegfa signal.
Chemical Information
-
CAS No. 2506273-81-8
-
Appearance Solid
-
Molecular Weight 389.37
-
Formula C21H18F3NO3
-
Color White to light brown
-
SMILES
OC[C@@H](C)NC(C(C=C1)=CC2=C1C(OC3=CC=C(C=C3)C(F)(F)F)=CC=C2)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (256.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
-
Data Sheet (274 KB)
-
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)
-
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5683 mL | 12.8413 mL | 25.6825 mL | 64.2063 mL |
| 5 mM | 0.5137 mL | 2.5683 mL | 5.1365 mL | 12.8413 mL | |
| 10 mM | 0.2568 mL | 1.2841 mL | 2.5683 mL | 6.4206 mL | |
| 15 mM | 0.1712 mL | 0.8561 mL | 1.7122 mL | 4.2804 mL | |
| 20 mM | 0.1284 mL | 0.6421 mL | 1.2841 mL | 3.2103 mL | |
| 25 mM | 0.1027 mL | 0.5137 mL | 1.0273 mL | 2.5683 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8561 mL | 2.1402 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6421 mL | 1.6052 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5137 mL | 1.2841 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0701 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8026 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6421 mL |
VT3989 Related Classifications
HY-400902 Related Classifications
Powered by Bioz
- VT3989
- 2506273-81-8
- VT 3989
- VT-3989
- YAP
- VEGFR
- Hippo (MST)
- merlin-depleted Schwann cells
- human-derived schwannoma cells
- YAP/TAZ-TEAD complex
- epithelioid hemangioendothelioma
- malignant pleural mesothelioma
- neurofibromatosis type 2
- vestibular schwannoma
- NF2-loss meningioma cells
- TEAD transcription factors
- EGFR mutant non-small cell lung cancer
- Inhibitor
- inhibitor
- inhibit