| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Tamatinib besylate (formerly R-406 besylate; prodrug of R 406) is a novel, potent and ATP-competitive inhibitor of spleen tyrosine kinase/Syk with potential anti-inflammatory activity. In cell-free assays, it inhibits Syk with an IC50 of 41 nM. Syk is essential for the signaling that activates B-cell receptors (BCR) and Fc receptors. Tamatinib is five times less effective against Flt3 and significantly inhibits Syk but not Lyn. It may be used to treat rheumatoid arthritis, other autoimmune diseases, and the inflammation linked to bronchial asthma caused by allergen-induced airway hyperresponsiveness (AHR).
| Targets |
Syk (Ki = 30 nM); Syk (IC50 = 41 nM); Lyn (IC50 = 63 nM); Lck (IC50 = 37 nM); FLT3
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
R406 is serially diluted in DMSO, diluted in kinase buffer (20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL acetylated BGG) and finally diluted to 1% DMSO by volume. After adding ATP and substrate to kinase buffer at room temperature, the final DMSO concentration is 0.2%. 0.125 ng of Syk is added to kinase buffer to initiate the kinase reactions, which are carried out in a final volume of 20 mL with 5 mM HS1 peptide substrate and 4 mM ATP. The reaction is left to continue at room temperature for forty minutes. 20 mL of PTK quench mix containing EDTA, anti-phosphotyrosine antibody (1X final), and fluorescent phosphopeptide tracer (0.5X final) diluted in FP Dilution Buffer is added to stop the reaction. A Polarion fluorescence polarization plate reader is used to read the plate after it has been incubated for 30 minutes at room temperature in the dark. Through competition with the phosphopeptide competitor included in the Tyrosine Kinase Assay Kit, a calibration curve is created that is used to convert data into the amount of phosphopeptide present. Non-linear regression analysis is used to fit the curve and test R406 at eleven different concentrations in order to determine the IC5
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| Cell Assay |
R406 is applied in serial dilutions (0.3, 0.6, 1.25, 2.5, or 5 μM) to DLBCL cell lines for either 72 or 96 hours. After that, the MTT assay is used to measure cellular proliferation, and the annexin V–FITC/propidium iodide (PI) staining is used to evaluate cell apoptosis. Cells are lysed, size-fractionated using polyacrylamide gel electrophoresis (PAGE), and immunoblotted to determine the presence of caspase 9, 8, and 3.
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| Animal Protocol |
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| References |
| Molecular Formula |
C28H29FN6O8S
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|---|---|
| Molecular Weight |
628.63
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| Exact Mass |
628.17516124
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| Elemental Analysis |
C, 53.50; H, 4.65; F, 3.02; N, 13.37; O, 20.36; S, 5.10
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| CAS # |
841290-81-1
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| Related CAS # |
R406 free base;841290-80-0
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| Appearance |
Solid powder
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| SMILES |
CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O
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| InChi Key |
UXDRJPYSTZHIOE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23FN6O5.C6H6O3S/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4;7-10(8,9)6-4-2-1-3-5-6/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30);1-5H,(H,7,8,9)
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| Chemical Name |
benzenesulfonic acid;6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
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| Synonyms |
R406 benzenesulfonate; R-406 benzenesulfonate; R-406 besylate; R406; R-406; R 406; R 406 besylate; R406 besylate; R406 benzenesulfonate; Tamatinib
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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 |
| 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) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5908 mL | 7.9538 mL | 15.9076 mL | |
| 5 mM | 0.3182 mL | 1.5908 mL | 3.1815 mL | |
| 10 mM | 0.1591 mL | 0.7954 mL | 1.5908 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.
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The Syk inhibitor R406 induces CLL cell apoptosis and abrogates BCR-derived survival signals. Blood. 2009 Jul 30; 114(5): 1029–1037. |
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