PRT-060318 2HCl

Catalog No.S7738 Batch:S773801

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Technical Data

Formula

C18H24N6O.2HCl
Molecular Weight 413.34 CAS No. 1194961-19-7(freebase)
Solubility (25°C)* In vitro DMSO 75 mg/mL (181.44 mM)
Water 75 mg/mL (181.44 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
water
75.0mg/ml Taking the 1 mL working solution as an example, add 75 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].

Protocol (from reference)

Cell Assay:

[4]
  • 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.
Animal Study:

[1]
  • Animal Models

    C57Bl/6 Mice; transgenic HIT mice

  • Dosages

    30 mg/kg

  • Administration

    orally via gavage

Selleck's PRT-060318 2HCl has been cited by 8 publications

Multi-phased Kinetics and Interaction of Protein Kinase Signaling in Glycoprotein VI-Induced Platelet αIIbβ3 Integrin Activation and Degranulation [ Thromb Haemost, 2024, 10.1055/a-2311-0117] PubMed: 38653482
D-dimer and CoV-2 spike-immune complexes contribute to the production of PGE2 and proinflammatory cytokines in monocytes [ PLoS Pathog, 2022, 18(4):e1010468] PubMed: 35385545
IgG-aggregates rapidly upregulate FcgRI expression at the surface of human neutrophils in a FcgRII-dependent fashion: A crucial role for FcgRI in the generation of reactive oxygen species [ FASEB J, 2020, 34(11):15208-15221] PubMed: 32946139
cAMP- and cGMP-elevating agents inhibit GPIbα-mediated aggregation but not GPIbα-stimulated Syk activation in human platelets. [ Cell Commun Signal, 2019, 17(1):122] PubMed: 31519182
SYK Targeting Represents a Potential Therapeutic Option for Relapsed Resistant Pediatric ETV6-RUNX1 B-Acute Lymphoblastic Leukemia Patients [ Int J Mol Sci, 2019, 20(24)E6175] PubMed: 31817853
Low catalase expression confers redox hypersensitivity and identifies an indolent clinical behavior in CLL [Cavallini C Blood, 2018, 131(17):1942-1954] PubMed: 29467184
Stress Granules Modulate SYK to Cause Microglial Cell Dysfunction in Alzheimer's Disease. [Ghosh S, et al. EBioMedicine, 2015, 2(11):1785-98] PubMed: 26870803
Stress Granules Modulate SYK to Cause Microglial Cell Dysfunction in Alzheimer's Disease [Hammitzsch A EBioMedicine, 2015, 2(11):1785-98] PubMed: 26870803

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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