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Technical Data
| Formula | C16H13FN4O2 |
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| Molecular Weight | 312.30 | CAS No. | 575474-82-7 | |
| Solubility (25°C)* | In vitro | DMSO | 62 mg/mL (198.52 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM. | ||
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| Targets |
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| In vitro | R112 inhibits degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC50] = 353 nmol/L) or basophils (histamine release, EC50 = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC50 = 490 nmol/L). R112 also blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action is immediate, and the inhibition is reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 does not inhibit phosphorylation of the Lyn target Syk (Y352), but inhibits the phosphorylation of the Syk target LAT (Y191), indicating that Syk kinase is the primary target of R112. Most phosphorylation events downstream of Syk are inhibited with similar potency by R112. In vitro kinase assays do not always correlate with the corresponding activity inside cells. R112 inhibits the Lyn kinase in vitro assay with an IC50 of 0.3 μmol/L; however, as mentioned previously, in CHMCs (Cultured human mast cells), R112 does not inhibit the phosphorylation of Syk (Y352), and therefore most likely does not inhibit Lyn activity[1]. |
Protocol (from reference)
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.