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P505-15 (also known as PRT062607) is a highly specific and potent, orally bioavailable small molecule spleen tyrosine kinase (Syk) inhibitor (IC50 = 1 nM) with anti-Syk activity that is at least 80-fold greater than its affinity for other kinases. P505-15 potently inhibited B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM) in human whole blood. Similar levels of ex vivo inhibition were measured after dosing in mice (Syk signaling IC50 0.32 μM). P505-15 (PRT062607) decreased cell viability in NHL and CLL. Oral administration of P505-15 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. In addition, combination treatment of primary CLL cells with P505-15 plus fludarabine produced synergistic enhancement of activity at nanomolar concentrations.
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Source | J Pharmacol Exp Ther (2013). Figure 1. P505-15 |
| Method | flow cytometry | |
| Cell Lines | Ramos cells | |
| Concentrations | 2 μM | |
| Incubation Time | 72 h | |
| Results | These data are consistent with previous observations that P505-15 is a selective and potent inhibitor of Syk, with no appreciable activity against other BCR-related kinases |
| Molecular Weight | 429.91 |
| Formula | C19H23N9O.HCl |
| CAS Number | 1370261-97-4 |
| Solubility (25°C) | DMSO 80 mg/mL Water 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Syk Products |
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| R-406
R406 is an orally bioavailable and selective inhibitor of spleen tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30 nM. |
| Fostamatinib disodium
Fostamatinib disodium (R788, R-935788) is a potent, ATP-competitive and selective Syk (Spleen tyrosine kinase) inhibitor with IC50 of 41 nM. |
| Fostamatinib
Fostamatinib (R788) is a spleen tyrosine kinase (Syk) inhibitor with IC50 of 41 nM. |
| GS-9973
GS-9973 is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM. |
| Piceatannol
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn. |
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