الصفحة الرئيسية>>Signaling Pathways>> Tyrosine Kinase>> Spleen Tyrosine Kinase (Syk)>>PRT-060318

PRT-060318 (Synonyms: P142-76, PRT318)

رقم الكتالوجGC11321

PRT-060318 (PRT318) هو مثبط انتقائي جديد لـ tyrosine kinase Syk مع IC 50 من 4 نانومتر

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PRT-060318 التركيب الكيميائي

Cas No.: 1194961-19-7

الحجم السعر المخزون الكميّة
10mM (in 1mL Water)
89٫00
متوفر
5mg
90٫00
متوفر
10mg
137٫00
متوفر
25mg
274٫00
متوفر
50mg
446٫00
متوفر
100mg
713٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

IC50: 4 nM

PRT-060318 is a novel Syk inhibitor.

Heparin-induced thrombocytopenia is a heparin therapy complication in which IgG antibodies against the platelet factor 4-heparin complex activate platelets. The FcγRIIA clustering initiates signaling cascades involving tyrosine kinases, such as spleen tyrosine kinase (Syk).

In vitro: PRT-060318 was identified as a potent inhibitor of purified Syk kinase. Syk kinase was inhibited by 92%, while the activities all other kinases retained more than 70% when PRT-060318 were evaluated at a concentration of 50 nM in a broad panel of kinase enzyme assays. In addition, PRT-060318 could dose-responsively inhibited convulxin-induced human PRP aggregation. Moreover, it was found that PRT-060318 was able to dose-responsively inhibit the increases in intracellular calcium in convulxin-treated platelets [1].

In vivo: Animal study showed that in contrast to vehicle-treated mice developed the expected thrombocytopenia, PRT-060318-treated mice had no significant change in platelet counts after injection of heparin. Moreover, the nadir platelet counts of PRT-060318-treated mice were found to be significantly higher than control mice. The PRT-060318-treated mice showed no bleeding diathesis or other adverse effects. In addition, PRT-060318 treatment in crush thrombosis model resulted in significant inhibition of platelet deposition without changing bleeding time [1].

Clinical trial: Up to now, PRT-060318 is still in the preclinical development stage.

Reference:
[1] Reilly MP,Sinha U,André P,Taylor SM,Pak Y,Deguzman FR,Nanda N,Pandey A,Stolla M,Bergmeier W,McKenzie SE.  PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. Blood.2011 Feb 17;117(7):2241-6.

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