Utatrectinib
Based on 1 Customer Validation
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.72%
- No. CAS: 1079274-94-4
- Fòrmula: C18H19FN8O
- Peso molecular:382.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
Utatrectinib (100 nM, 22 h) inhibits the migration of TrkC-expressing U2SO cells[2].
Utatrectinib (1-10 nM, 24 h) inhibits cell growth in KM12, H460 and H810 cells[3].
Utatrectinib (5 nM, 24 h) inhibits phosphorylation of TRKA/B and downstream signaling in KM12, H460 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TrkC-expressing U2SO cells
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Concentration:100 nM
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Incubation Time:22 h
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Result:Inhibited cell migration (~2.3-fold, P<0.01).
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Cell Line:KM12, H460 cells
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Concentration:0, 1, 5 nM
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Incubation Time:24 h
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Result:Inhibited pTRKA Tyr490 and pAk in KM12 cells.
Inhibited pTRKB Tyr706/707 and pERK in H460 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenograft nu/nu mice models of human ACC: ACCX6 and ACCX9[2]
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Dosage:50 mg/kg
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Administration:Oral administration, daily.
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Result:Tumor growth inhibition (TGI): 64% (in ACCX6 model)
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1079274-94-4
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Appearance Solid
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Peso molecular 382.39
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Fòrmula C18H19FN8O
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Color Blue to blue-green
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SMILES
CC(C)OC1=CC(N2C=NC3=CC=C(N[C@H](C4=NC=C(F)C=N4)C)N=C32)=NN1
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Synonyms
AZD-7451
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (130.76 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. 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: ≥ 1.25 mg/mL (3.27 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (3.27 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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 (273 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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Instrucciones de manejo (2659 KB)
Referencias
[2]. Ivanov SV, et al. TrkC signaling is activated in adenoid cystic carcinoma and requires NT-3 to stimulate invasive behavior. Oncogene. 2013 Aug 8;32(32):3698-710. [Content Brief]
[3]. Tatematsu T, et al. Investigation of neurotrophic tyrosine kinase receptor 1 fusions and neurotrophic tyrosine kinase receptor family expression in non-small-cell lung cancer and sensitivity to AZD7451 in vitro. Mol Clin Oncol. 2014 Sep;2(5):725-730. [Content Brief]
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 | 2.6151 mL | 13.0757 mL | 26.1513 mL | 65.3783 mL |
| 5 mM | 0.5230 mL | 2.6151 mL | 5.2303 mL | 13.0757 mL | |
| 10 mM | 0.2615 mL | 1.3076 mL | 2.6151 mL | 6.5378 mL | |
| 15 mM | 0.1743 mL | 0.8717 mL | 1.7434 mL | 4.3586 mL | |
| 20 mM | 0.1308 mL | 0.6538 mL | 1.3076 mL | 3.2689 mL | |
| 25 mM | 0.1046 mL | 0.5230 mL | 1.0461 mL | 2.6151 mL | |
| 30 mM | 0.0872 mL | 0.4359 mL | 0.8717 mL | 2.1793 mL | |
| 40 mM | 0.0654 mL | 0.3269 mL | 0.6538 mL | 1.6345 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5230 mL | 1.3076 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4359 mL | 1.0896 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3269 mL | 0.8172 mL | |
| 100 mM | 0.0262 mL | 0.1308 mL | 0.2615 mL | 0.6538 mL |
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