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Potent inhibitor of lymphocyte specific kinase (Lck). IC50 values are 0.007, 0.021, 0.042 and 0.20 μM for Lck, Lyn, Src and Syk kinases respectively. Displays >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Inhibits T cell proliferation in vitro and inhibits arthritis in two in vivo models. Orally active.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|ethanol||5.31||10 with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 530.62. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.88 mL||9.42 mL||18.85 mL|
|5 mM||0.38 mL||1.88 mL||3.77 mL|
|10 mM||0.19 mL||0.94 mL||1.88 mL|
|50 mM||0.04 mL||0.19 mL||0.38 mL|
References are publications that support the biological activity of the product.
Martin et al (2008) Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory J.Med.Chem. 51 1637 PMID: 18278858
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Keywords: TC-S 7003, TC-S 7003 supplier, Lck, kinases, inhibitors, inhibits, lymphocyte, specific, Src, Kinases, 3567, Tocris Bioscience
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