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PRT-060318

Cat. No. M5252
PRT-060318 Structure
Synonym:

PRT318

Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 220 In stock
50mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.

In vivo: In both rabbit and pig models, intravenous infusion of PRT060318 targets maximal inhibition of Syk kinase activity and significantly inhibits arterial thrombosis. The antithrombotic activity of PRT060318 in pigs is remarkable because it was achieved with complete inhibition of CVXN-induced platelet aggregation, with no effect on ADP-induced platelet aggregation, and no prolongation of ear bleeding time.

Also, Syk inhibitor PRT318 is an active agent in HIT. Inhibition of Syk signaling with the orally bio-available PRT318 limits the thrombocytopenic and thrombotic effects of HIT IC in vivo.

Protocol
Cell Experiment
Cell lines LY3,LY4,LY7,LY18 cell lines
Preparation method The numbers of cells treated with various doses of PRT318 are followed over time. PRT318 inhibits growth of the sensitive cell lines in a dose-dependent manner. Two sensitive (LY7 and LY18) and 2 resistant (LY3 and LY4) cell lines are treated with indicated doses of PRT318.
Concentrations 0-3μM
Incubation time 0-72h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 413.34
Formula C18H24N6O.2HCl
CAS Number 1194961-19-7 (free base)
Purity >99%
Solubility 75 mg/mL in DMSO
Storage at -20°C
References

Src family kinases and Syk are required for neutrophil extracellular trap formation in response to β-glucan particles.
Nanì S, et al. J Innate Immun. 2015;7(1):59-73. PMID: 25277753.

PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model.
Reilly MP, et al. Blood. 2011 Feb 17;117(7):2241-6. PMID: 21088136.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PRT-060318, PRT318 supplier, Syk, inhibitors

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