Bozitinib
Based on 1 publication(s) in Google Scholar
Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
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- Pureza: 98.88%
- No. CAS: 1440964-89-5
- Fòrmula: C20H15F3N8
- Peso molecular:424.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bozitinib
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Actividad biológica
Bozitinib (PLB-1001) (30 μM; 6 hours) inhibits the phosphorylation of MET and STAT3, has a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human astrocytes (HA) cells
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Concentration:30 μM
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Incubation Time:6 hours
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Result:Decreased p-STAT3,p-MET expression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1440964-89-5
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Appearance Solid
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Peso molecular 424.38
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Fòrmula C20H15F3N8
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Color Light yellow to yellow
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SMILES
CN1N=C2C=C(F)C(C(C3=NN=C4C=CC(C5=CN(C6CC6)N=C5)=NN43)(F)F)=CC2=C1
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Synonyms
PLB-1001; CBT-101; Vebreltinib
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]2023 Feb 21;4(2):100911. PMID: 36657446
Solvente y solubilidad
DMSO : 50 mg/mL (117.82 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in 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 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 (393 KB)
- English - EN (393 KB)
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- Norwegian - NO (393 KB)
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- Swedish - SV (393 KB)
- Italian - IT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.3564 mL | 11.7819 mL | 23.5638 mL | 58.9095 mL |
| 5 mM | 0.4713 mL | 2.3564 mL | 4.7128 mL | 11.7819 mL | |
| 10 mM | 0.2356 mL | 1.1782 mL | 2.3564 mL | 5.8909 mL | |
| 15 mM | 0.1571 mL | 0.7855 mL | 1.5709 mL | 3.9273 mL | |
| 20 mM | 0.1178 mL | 0.5891 mL | 1.1782 mL | 2.9455 mL | |
| 25 mM | 0.0943 mL | 0.4713 mL | 0.9426 mL | 2.3564 mL | |
| 30 mM | 0.0785 mL | 0.3927 mL | 0.7855 mL | 1.9636 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5891 mL | 1.4727 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4713 mL | 1.1782 mL | |
| 60 mM | 0.0393 mL | 0.1964 mL | 0.3927 mL | 0.9818 mL | |
| 80 mM | 0.0295 mL | 0.1473 mL | 0.2945 mL | 0.7364 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5891 mL |
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