TEAD1/3/4-IN-1
Based on 1 Customer Validation
TEAD1/3/4-IN-1 is an orally active inhibitor of TEAD1/3/4. TEAD1/3/4-IN-1 inhibits the YAP/TAZ-TEAD interaction, with its EC50 being 2 nM. TEAD1/3/4-IN-1 has anti-proliferative activity against NCI-H226 cells. TEAD1/3/4-IN-1 can be used in the research of lung squamous cell carcinoma.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 2762619-63-4
- Formula: C18H13F4N5O2
- Molecular Weight:407.32
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Storage:Powder -20°C, 3 years , 4°C, 2 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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All YAP Isoforms
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Biological Activity
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YAP/TAZ-TEAD 2 nM (EC50) |
TEAD1/3/4-IN-1 (Compound 1) (0-20 μM, 6 days) inhibits the proliferation of NCI-H226 cells, with its IC50 being 7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | AUClast |
|---|---|---|---|---|
| Mice | 5 mg/kg | p.o. | 1967 ng/mL | 17195 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H226 pulmonary squamous cell carcinoma xenograft model established in female BALB/c nude (6-7 weeks)[1]
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Dosage:10 and 50 mg/kg
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Administration:Oral administration (p.o.), once daily for 45 days
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Result:Exhibited significant anti-tumor activity and the TGI values were 109% and 111% in 10 mg/kg and 50 mg/kg groups.
Chemical Information
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CAS No. 2762619-63-4
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Appearance Solid
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Molecular Weight 407.32
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Formula C18H13F4N5O2
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Color Light yellow to yellow
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SMILES
O=C(N1CC(C1)N2C(N(C3=NC=CN=C32)C4=CC=C(C(F)(F)F)C=C4)=O)C(F)=C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 27.5 mg/mL (67.51 mM; ultrasonic and warming and heat to 60°C; 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. 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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 2.4551 mL | 12.2754 mL | 24.5507 mL | 61.3768 mL |
| 5 mM | 0.4910 mL | 2.4551 mL | 4.9101 mL | 12.2754 mL | |
| 10 mM | 0.2455 mL | 1.2275 mL | 2.4551 mL | 6.1377 mL | |
| 15 mM | 0.1637 mL | 0.8184 mL | 1.6367 mL | 4.0918 mL | |
| 20 mM | 0.1228 mL | 0.6138 mL | 1.2275 mL | 3.0688 mL | |
| 25 mM | 0.0982 mL | 0.4910 mL | 0.9820 mL | 2.4551 mL | |
| 30 mM | 0.0818 mL | 0.4092 mL | 0.8184 mL | 2.0459 mL | |
| 40 mM | 0.0614 mL | 0.3069 mL | 0.6138 mL | 1.5344 mL | |
| 50 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2275 mL | |
| 60 mM | 0.0409 mL | 0.2046 mL | 0.4092 mL | 1.0229 mL |
TEAD1/3/4-IN-1 Related Classifications
HY-174275 Related Classifications
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