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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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| GSK143
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. |
| PRT062607
PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70. |
| GSK143 dihydrochloride
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. |
| Syk Kinase Peptide Substrate
Syk Kinase Peptide Substrate is a Syk kinase peptide substrate. |
| TOP1288
TOP1288 is an SRC/Syk/p38α inhibitor for studies related to ulcerative colitis. |
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