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PRT-060318

Catalog No.
B6161
novel Syk inhibitor
Grouped product items
SizePriceStock Qty
5mg
$125.00
In stock
10mg
$198.00
In stock
25mg
$397.00
In stock
50mg
$647.00
In stock
100mg
$1,034.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt449.81
Cas No.1194961-19-7
FormulaC18H27Cl3N6O
Solubility≥45.7 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide
SDFDownload SDF
Canonical SMILESO=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

PRT-060318