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    InvivoChem Cat #: V0637
    CAS #: 1493764-08-1Purity ≥98%

    Description: UNC2881 (UNC-2881) is a novel, potent and specific Mer tyrosine kinase inhibitor with potential utility for prevention and treatment of pathologic thrombosis. It inhibits Mer with an IC50 of 4.3 nM, and shows 83- and 58-fold higher selectivity over Axl and Tyro3, respectively. The role of Mer kinase in regulating the second phase of platelet activation generates an opportunity to use Mer inhibitors for preventing thrombosis with diminished likelihood for bleeding as compared to current therapies. 

    References: J Med Chem. 2013 Dec 12;56(23):9693-700.

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    Molecular Weight (MW)463.58
    CAS No.1493764-08-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 292 mg/mL (198.5 mM)   
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (10.8 mM)
    Other info
    Chemical Name: N-(4-(1H-imidazol-1-yl)benzyl)-2-(butylamino)-4-(((1r,4r)-4-hydroxycyclohexyl)amino)pyrimidine-5-carboxamide
    InChi Code: InChI=1S/C25H33N7O2/c1-2-3-12-27-25-29-16-22(23(31-25)30-19-6-10-21(33)11-7-19)24(34)28-15-18-4-8-20(9-5-18)32-14-13-26-17-32/h4-5,8-9,13-14,16-17,19,21,33H,2-3,6-7,10-12,15H2,1H3,(H,28,34)(H2,27,29,30,31)/t19-,21-
    SMILES Code: O=C(C1=CN=C(NCCCC)N=C1N[[email protected]]2CC[[email protected]](O)CC2)NCC3=CC=C(N4C=CN=C4)C=C3 
    SynonymsUNC-2881, UNC 2881, UNC2881, 

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    In Vitro

    In vitro activity: UNC2881 inhibits Mer kinase activity in 697 B-ALL cells with IC50 of 22 nM, and inhibits collagen-stimulated platelet aggregation.

    Kinase Assay: UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.

    Cell Assay: In 697 B-ALL cells, UNC2881 inhibited Mer phosphorylation with IC50 value of 22 nM. Also, UNC2881 inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the intracellular domain of Mer and the extracellular domain of the epidermal growth factor receptor (EGFR). In human platelet-rich plasma, UNC2881 inhibited platelet aggregation induced by fibrillar Type I equine collagen by greater than 25%. UNC2881 also inhibited ATP release, a marker of platelet activation.

    In VivoUNC2881 have high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability in mice.
    Animal modelMouse model
    Formulation & Dosage94.5 mL/min/kg; oral
    ReferencesJ Med Chem. 2013 Dec 12;56(23):9693-700.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    UNC2881 (compound 23) inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells. J Med Chem. 2013 Dec 12;56(23):9693-700.



    23 inhibits ligand-stimulated activation of a chimeric EGFR-MerTK. J Med Chem. 2013 Dec 12;56(23):9693-700.


    23 inhibits collagen-stimulated platelet aggregation. J Med Chem. 2013 Dec 12;56(23):9693-700.


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