Enbezotinib
Based on 1 publication(s) in Google Scholar
Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 2359649-81-1
- Formula: C21H21FN6O3
- Molecular Weight:424.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Enbezotinib
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Biological Activity
RET[1]
Enbezotinib (compound 5) (0.3-300 nM) inhibits p-RET (y905) in RET-driven cells[1].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2359649-81-1
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Appearance Solid
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Molecular Weight 424.43
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Formula C21H21FN6O3
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Color White to off-white
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SMILES
FC(C=C1CN2C3=NC4=C5C=NN4C=C3O[C@]6([H])[C@@]2([H])CCC6)=CN=C1O[C@@H](C)CNC5=O
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Synonyms
TPX-0046
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]2025 Jun 7:2025.06.04.657911. PMID: 40502048
Solvent & Solubility
DMSO : 100 mg/mL (235.61 mM; ultrasonic and warming and heat to 80°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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (280 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)
- 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 | 2.3561 mL | 11.7805 mL | 23.5610 mL | 58.9025 mL |
| 5 mM | 0.4712 mL | 2.3561 mL | 4.7122 mL | 11.7805 mL | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3561 mL | 5.8903 mL | |
| 15 mM | 0.1571 mL | 0.7854 mL | 1.5707 mL | 3.9268 mL | |
| 20 mM | 0.1178 mL | 0.5890 mL | 1.1781 mL | 2.9451 mL | |
| 25 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3561 mL | |
| 30 mM | 0.0785 mL | 0.3927 mL | 0.7854 mL | 1.9634 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5890 mL | 1.4726 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1781 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3927 mL | 0.9817 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2945 mL | 0.7363 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5890 mL |