Home Angiogenesis Syk inhibitor PRT-060318 2HCl For research use only.

PRT-060318 2HCl

Synonyms: PRT318

PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.

PRT-060318 2HCl Chemical Structure

PRT-060318 2HCl Chemical Structure

CAS No. 1194961-19-7(freebase)

Purity & Quality Control

Batch: S773801 DMSO]75 mg/mL]false]Water]75 mg/mL]false]Ethanol]Insoluble]false Purity: 99.08%
99.08

PRT-060318 2HCl Related Products

Signaling Pathway

Syk Signaling Pathways

Syk Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
ramos cells Function assay Inhibition of Erk1/2 phosphorylation expressed in ramos cells after 30 mins by MSD assay, IC50=0.01585 μM 21903390
primary B cells Function assay Immunomodulatory activity in human primary B cells assessed as induction of CD69 expression after 24 hrs by FITC-conjugated flow cytometry, IC50=0.63096 μM 11493841
CHO-K1 cells Function assay 2 h Inhibition of human ERG expressed in CHO-K1 cells after 2 hrs by Cy3b-Dofetilide-based fluorescence polarisation assay 21903390
Click to View More Cell Line Experimental Data

Biological Activity

Description PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
Targets
Syk [1]
(Cell-free assay)
4nM
In vitro
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].
Cell Research Cell lines LY3，LY4，LY7,LY18 cell lines
Concentrations 0-3μM
Incubation Time 0-72h
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.
In Vivo
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].
Animal Research Animal Models C57Bl/6 Mice; transgenic HIT mice
Dosages 30 mg/kg
Administration orally via gavage

Chemical Information & Solubility

Molecular Weight 413.34 Formula

C18H24N6O.2HCl
CAS No. 1194961-19-7(freebase) SDF Download PRT-060318 2HCl SDF
Smiles CC1=CC(=CC=C1)NC2=NC(=NC=C2C(=O)N)NC3CCCCC3N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (181.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 75 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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