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    UNC2250
    UNC2250

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0636
    CAS #: 1493694-70-4Purity ≥98%

    Description: UNC2250 (UNC-2250) is a novel, potent and selective Mer inhibitor with potential antitumor activity. It inhibits Mer with an IC50 of 1.7 nM, and shows about 160- and 60-fold higher selectivity for inhibiting Mer over other closely related kinases such as Axl/Tyro3. UNC2250 demonstrates high anti-proliferative activity in vitro and in vivo antitumor efficacy as well. 

    References: J Med Chem. 2013 Dec 12;56(23):9683-92.

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    Molecular Weight (MW)440.58
    FormulaC24H36N6O2
    CAS No.1493694-70-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 2 mg/mL (4.5 mM)    
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other infoChemical Name: (1r,4r)-4-((2-(butylamino)-5-(5-(morpholinomethyl)pyridin-2-yl)pyrimidin-4-yl)amino)cyclohexanol
    InChi Key: HSYSSKFCQHXOBP-MXVIHJGJSA-N
    InChi Code: InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)/t19-,20-
    SMILES Code: O[[email protected]]1CC[[email protected]](NC2=NC(NCCCC)=NC=C2C3=NC=C(CN4CCOCC4)C=C3)CC1
    SynonymsUNC-2250, UNC 2250, UNC2250, 


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    In Vitro

    In vitro activity: UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells.


    Kinase Assay: Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software.


    Cell Assay: BT-12 rhabdoid tumor cells (10 000 cells) are cultured in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted after 3 weeks. Colo699 NSCLC cells (15 000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.

    In VivoAccording to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility.
    Animal modelMice or rat
    Formulation & DosageN/A
    References

    J Med Chem. 2013 Dec 12;56(23):9683-92.


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

    UNC2250

    X-ray structure of 3 in complex with Mer kinase domain (PDB ID Code: 4M3Q). J Med Chem. 2013 Dec 12;56(23):9683-92.

    UNC2250

    Kinase tree. J Med Chem, 2013. 56(23): p. 9683-92.

    UNC2250

    10 inhibits Mer tyrosine kinase activation in acute leukemia cells. J Med Chem. 2013 Dec 12;56(23):9683-92.


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