Home Angiogenesis Syk inhibitor PRT-060318 2HCl

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PRT-060318 2HCl Syk inhibitor

Cat.No.S7738

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 Syk inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 413.34

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Quality Control

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

Cell Culture, Treatment & Working Concentration

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
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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (181.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 75 mg/mL

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 413.34 Formula

C18H24N6O.2HCl

 Storage (From the date of receipt)
CAS No. 1194961-19-7(freebase) Download SDF Storage of Stock Solutions

Synonyms PRT318 Smiles CC1=CC(=CC=C1)NC2=NC(=NC=C2C(=O)N)NC3CCCCC3N

Mechanism of Action

Targets/IC50/Ki
Syk
(Cell-free assay)
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. 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/22025527/

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