Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Dasatinib N-oxide is a major and N-oxidated metabolite of Dasatinib (BMS354825; Sprycel), which is an approved anticancer drug acting as a dual Bcr-Abl and Src kinase inhibitor. It is also an impurity during the production of dasatinib.
ln Vivo |
Following oral treatment, dasatinib N-oxide is a metabolite that exhibits pharmacological activity [1].
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References |
[1]. Christopher LJ, et, al. Metabolism and disposition of dasatinib after oral administration to humans. Drug Metab Dispos. 2008 Jul;36(7):1357-64.
[2]. Furlong MT, et, al. A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma: application to a clinical pharmacokinetic study. J Pharm Biomed Anal. 2012 |
Molecular Formula |
C22H26N7O3SCL
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Molecular Weight |
504.01
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Exact Mass |
503.1506
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Elemental Analysis |
C, 52.43 H, 5.20 Cl, 7.03 N, 19.45 O, 9.52 S, 6.36
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CAS # |
910297-52-8
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Related CAS # |
Dasatinib N-oxide-d8;1189988-36-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
OCCN(CCN1C2=CC(NC3=NC=C(C(NC4=C(Cl)C=CC=C4C)=O)S3)=NC(C)=N2)(CC1)=O
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InChi Key |
UEFNEEZCTQCRAW-UHFFFAOYSA-N
InChi Code
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Chemical Name |
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-4-oxido-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
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Synonyms |
BMS-354825 N-oxide
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~8.33 mg/mL (~16.53 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.65 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9841 mL | 9.9204 mL | 19.8409 mL | |
5 mM | 0.3968 mL | 1.9841 mL | 3.9682 mL | |
10 mM | 0.1984 mL | 0.9920 mL | 1.9841 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.