N-Deshydroxyethyl Dasatinib
Based on 1 Customer Validation
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
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- Pureté: 97.19%
- CAS No.: 910297-51-7
- Formule: C20H22ClN7OS
- Masse moléculaire:443.95
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
|
c-Src |
Lck |
| Analyte | Cmax (ng/mL) | AUC0-t (h*ng/mL) | AUC0-inf (h*ng/mL) | Tmax (h) | T1/2 (h) | Kel (h-1) |
| N-Deshydroxyethyl Dasatinib | 2.05 | 8.7 | 23.9 | 2.0 | 10.293 | 0.072 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 910297-51-7
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Appearance Solid
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Masse moléculaire 443.95
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Formule C20H22ClN7OS
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Color White to off-white
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SMILES
O=C(C1=CN=C(NC2=NC(C)=NC(N3CCNCC3)=C2)S1)NC4=C(C)C=CC=C4Cl
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Synonyms
N-Deshydroxyethyl BMS-354825
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 55 mg/mL (123.89 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: ≥ 2.75 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (6.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (726 KB)
- English - EN (726 KB)
- Français - FR (726 KB)
- Deutsch - DE (726 KB)
- Norwegian - NO (726 KB)
- Español - ES (726 KB)
- Swedish - SV (726 KB)
- Italian - IT (726 KB)
- Portuguese - PT (726 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666. [Content Brief]
[2]. Thappali SR, et al. Simultaneous determination of methotrexate, dasatinib and its active metabolite N- deshydroxyethyl dasatinib in rat plasma by LC-MS/MS: method validation and application to pharmacokinetic study. Arzneimittelforschung. 2012 Dec;62(12):624-30. [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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2525 mL | 11.2625 mL | 22.5251 mL | 56.3126 mL |
| 5 mM | 0.4505 mL | 2.2525 mL | 4.5050 mL | 11.2625 mL | |
| 10 mM | 0.2253 mL | 1.1263 mL | 2.2525 mL | 5.6313 mL | |
| 15 mM | 0.1502 mL | 0.7508 mL | 1.5017 mL | 3.7542 mL | |
| 20 mM | 0.1126 mL | 0.5631 mL | 1.1263 mL | 2.8156 mL | |
| 25 mM | 0.0901 mL | 0.4505 mL | 0.9010 mL | 2.2525 mL | |
| 30 mM | 0.0751 mL | 0.3754 mL | 0.7508 mL | 1.8771 mL | |
| 40 mM | 0.0563 mL | 0.2816 mL | 0.5631 mL | 1.4078 mL | |
| 50 mM | 0.0451 mL | 0.2253 mL | 0.4505 mL | 1.1263 mL | |
| 60 mM | 0.0375 mL | 0.1877 mL | 0.3754 mL | 0.9385 mL | |
| 80 mM | 0.0282 mL | 0.1408 mL | 0.2816 mL | 0.7039 mL | |
| 100 mM | 0.0225 mL | 0.1126 mL | 0.2253 mL | 0.5631 mL |
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