PRT062607 (BIIB-057) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | In stock | $ 99 | |
| 2 mg | In stock | $ 168 | |
| 4 mg | In stock | $ 300 | |
| 10 mg | In stock | $ 470 | |
| 20 mg | In stock | $ 728 |
| Description | PRT062607 (BIIB-057) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases. |
| Targets&IC50 | Fgr: 81 nM (cell free), MLK1: 88 nM (cell free), Syk: 1 nM (cell free) |
| In vitro | NLC co-cultures were established by suspending PBMC from patients with CLL in complete RPMI medium with 10% fetal bovine serum and penicillin-streptomycin-glutamine to a concentration of 107 cells/mL (total 2 mL). Cells were incubated for 14 days in 24-well plates as previously described. To evaluate whether the Syk inhibitors PRT318 and P505-15 could overcome the protective effect of NLC, CLL cells were cultured under standardized conditions on NLC or in suspension, in the presence or absence of PRT318 and P505-15. At the indicated time points, CLL cells were collected and assayed for cell viability as previously described. |
| In vivo | All animal studies were performed in strict accordance with the Institutional Animal Care and Use Committee ethical guidelines. Female BALB/c mice received a single oral dose of 15 or 30 mg/kg P505-15 and were anesthetized with a subcutaneous ketamine cocktail, and blood was harvested via cardiac puncture at 0.5, 1, 2, 3, 4, 5, 6, 8, and 24 h postdose, (n = 3/time point; n = 8 vehicle controls). Blood was dispensed into three heparin-containing tubes, one for determination of drug concentration and the remaining two for ex vivo stimulation with isotype control or anti-mouse IgD antibody for 10 min. Blood was processed for intracellular phospho-flow cytometry to evaluate BCR signaling as described earlier; mouse B cells were detected by using CD45R-B220 PerCP-conjugated antibody. Plasma samples were analyzed for P505-15 concentration by using a liquid chromatography tandem mass spectrometer. The analytical range was 2 to 5000 ng/ml. |
| Synonyms | PRT062607 (P505-15, BIIB057) HCl, P505-15 Hydrochloride |
| CAS No. | 1370261-97-4 |
| Chemical Formula | C19H24ClN9O |
| Molecular Weight | 429.91 |
| Solubility | Ethanol: <1 mg/mL H2O: 79 mg/mL (183.8 mM); DMSO: 80 mg/mL (186.1 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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