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PRT-060318

Catalog No. T6957   CAS 1194961-19-7
Synonyms: P142-76, PRT318, PRT-060318 2HCl

PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.

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PRT-060318 Chemical Structure
PRT-060318, CAS 1194961-19-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 35.00
2 mg In stock $ 48.00
5 mg In stock $ 86.00
10 mg In stock $ 137.00
25 mg In stock $ 288.00
50 mg In stock $ 490.00
100 mg In stock $ 715.00
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Purity: 98.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.
Targets&IC50 Syk:4nM
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[1]. 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[2].
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[3]. 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[1].
Cell Research 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. (Only for Reference)
Synonyms P142-76, PRT318, PRT-060318 2HCl
Molecular Weight 340.42
Formula C18H24N6O
CAS No. 1194961-19-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 5.6 mg/mL (16.45 mM), sonification/heating is recommended.

TargetMolReferences and Literature

1. Reilly MP, et al. Blood. 2011, 117(7):2241-2246. 2. Hoellenriegel J, et al. Leukemia. 2012, 26(7):1576-1583. 3. Andre P, et al. Blood. 2011, 118(18):5000-5010. 4. Cheng S, et al. Blood. 2011, 118(24):6342-6352.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Preclinical Compound Library

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Cerdulatinib hydrochloride R406 free base Syk-IN-7 RO9021 MNS GSK1904529A Lanraplenib succinate Fostamatinib Disodium

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Keywords

PRT-060318 1194961-19-7 Angiogenesis Tyrosine Kinase/Adaptors Syk PRT-318 PRT 060318 P142-76 PRT318 PRT-060318 2HCl Inhibitor inhibit PRT 318 Spleen tyrosine kinase PRT060318 inhibitor

 

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