MYF-03-69
Based on 1 publication(s) in Google Scholar
MYF-03-69 (TEAD-IN-3) is a covalent and irreversible TEAD inhibitor with IC50s of 385, 143, 558 and 173 nM for TEAD1, TEAD2, TEAD3 and TEAD4. MYF-03-69 disrupts YAP-TEAD association, suppresses TEAD transcriptional activity (IC50 = 56 nM) and up-regulates apoptosis gene BMF. MYF-03-69 selectively inhibits mesothelioma cancer cells with defective Hippo signaling. MYF-03-69 can be used for the study of malignant pleural mesothelioma (MPM).
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- Pureza: 98.11%
- No. CAS: 2416418-11-4
- Fòrmula: C22H20F3N5O2
- Peso molecular:443.42
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
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Transcription Factor-Targeted Library
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Anti-Colorectal Cancer Compound Library
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Anti-Pulmonary Fibrosis Compound Library
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Cancer Stem Cells Compound Library
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Cysteine Targeted Covalent Library
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Highly Selective Inhibitors Library
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Highly Selective Activators Library
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Cell Death Library
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High-Throughput Bioactive Compound Library
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Publications Citing Use of MedChemExpress (MCE) MYF-03-69
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Actividad biológica
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TEAD1 385 nM (IC50) |
TEAD2 143 nM (IC50) |
TEAD3 558 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| NCI-H226 | IC50 |
63 nM
Compound: (+/-)-1
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Antiproliferative activity against human NCI-H226 cells assessed as reduction in cell viability measured for 5 days by celliter-glo assay
Antiproliferative activity against human NCI-H226 cells assessed as reduction in cell viability measured for 5 days by celliter-glo assay
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[PMID: 36946421] |
MYF-03-69 (0-10 μM, 5 days) selectively inhibits the proliferation of mesothelioma cells with defective Hippo signaling (such as NCI-H226, MSTO-211H), while having very little cytotoxicity towards normal mesothelial cells (MeT-5A) or cancer cells with intact Hippo signaling[1].
MYF-03-69 (0.1-10 μM, 48 h) induces G1 phase cell cycle arrest in NCI-H226 and MSTO-211H cells[1].
MYF-03-69 (0.1-2 μM, 24 h) inhibits palmitoylation of TEAD protein and disrupts its association with YAP in NCI-H226 cells[1].
MYF-03-69 (2 μM) downregulates YAP-TEAD target genes (such as CTGF, CYR61, and ANKRD1) and upregulates the pro-apoptotic gene BMF in NCI-H226 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H226 and MSTO-211H cells
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Concentration:0.1, 0.5, 2, 10 μM
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Incubation Time:48 h
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Result:Caused cell cycle arrest at the G1 phase.
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Cell Line:NCI-H226 and MSTO-211H cells
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Concentration:0.1, 0.5, 2 μM
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Incubation Time:24 h
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Result:Significantly decreased endogenous YAP coimmunoprecipitation with a pan-TEAD antibody, whereas this treatment had minimal effect on TEAD protein level.
Decreased protein level of CYR61 and AXL gene products.
Chemical Information
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No. CAS 2416418-11-4
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Appearance Solid
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Peso molecular 443.42
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Fòrmula C22H20F3N5O2
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Color Light yellow to yellow
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SMILES
FC(F)(F)C(C=C1)=CC=C1CO[C@H]2[C@@](N3C=C(C4=CN=CC=C4)N=N3)([H])CN(C2)C(C=C)=O
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Synonyms
TEAD-IN-3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 100 mg/mL (225.52 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (5.64 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 (5.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (278 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)
- 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 | 2.2552 mL | 11.2760 mL | 22.5520 mL | 56.3800 mL |
| 5 mM | 0.4510 mL | 2.2552 mL | 4.5104 mL | 11.2760 mL | |
| 10 mM | 0.2255 mL | 1.1276 mL | 2.2552 mL | 5.6380 mL | |
| 15 mM | 0.1503 mL | 0.7517 mL | 1.5035 mL | 3.7587 mL | |
| 20 mM | 0.1128 mL | 0.5638 mL | 1.1276 mL | 2.8190 mL | |
| 25 mM | 0.0902 mL | 0.4510 mL | 0.9021 mL | 2.2552 mL | |
| 30 mM | 0.0752 mL | 0.3759 mL | 0.7517 mL | 1.8793 mL | |
| 40 mM | 0.0564 mL | 0.2819 mL | 0.5638 mL | 1.4095 mL | |
| 50 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1276 mL | |
| 60 mM | 0.0376 mL | 0.1879 mL | 0.3759 mL | 0.9397 mL | |
| 80 mM | 0.0282 mL | 0.1409 mL | 0.2819 mL | 0.7047 mL | |
| 100 mM | 0.0226 mL | 0.1128 mL | 0.2255 mL | 0.5638 mL |
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