My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    UNC-2025
    UNC-2025

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V2549
    CAS #: 1429881-91-3Purity ≥98%

    Description: UNC-2025 is a novel, potent and orally bioavailable dual inhibitor of MER/FLT3 with IC50 of 0.74 nM and 0.8 nM, respectively, it displayed about 20-fold selectivity over Axl and Tyro3. UNC-2025 is capable of inhibiting Mer phosphorylation in vivo following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined. 

    References: J Med Chem. 2014 Aug 28;57(16):7031-41; Mol Cancer Ther. 2015 Sep;14(9):2014-22.

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)476.66
    FormulaC28H40N6O
    CAS No.1429881-91-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: > 5 mg/mL
    Water: < 4.9 mg/mL
    Ethanol: N/A
    SMILES CodeO[[email protected]]1CC[[email protected]](N2C=C(C3=CC=C(CN4CCN(C)CC4)C=C3)C5=CN=C(NCCCC)N=C52)CC1
    SynonymsUNC2025, UNC 2025, UNC2025, 

    Chemical Name: (1r,4r)-4-(2-(butylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol

    Exact Mass: 476.32636 


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: UNC-2025 is a novel, potent and orally bioavailable dual inhibitor of MER/FLT3 with IC50 of 0.74 nM and 0.8 nM, respectively, it displayed about 20-fold selectivity over Axl and Tyro3. UNC-2025 is capable of inhibiting Mer phosphorylation in vivo. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.  


    Kinase Assay: UNC2025 hydrochloride is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3. UNC2025 was capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that 11 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.


    Cell Assay: In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation.

    In VivoIn mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth
    Animal modelNOD/SCID/gamma mice bearing 697 acute leukemia tumor
    Formulation & DosageFormulated in 0.5% (w/v) NaCMC with 0.1% (v/v) Tween-80 in water;  3 mg/kg; Oral gavage
    ReferencesJ Med Chem. 2014 Aug 28;57(16):7031-41; Mol Cancer Ther. 2015 Sep;14(9):2014-22.


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

    UNC-2025

    UNC2025 inhibits colony formation in soft agar. Mol Cancer Ther. 2015 Sep;14(9):2014-22.

    UNC-2025

    UNC2025 Inhibits NSCLC tumor growth in vivo: H2228 (A) or A549 (B,C). Mol Cancer Ther. 2015 Sep; 14(9): 2014–2022.

    UNC-2025

    UNC2025 inhibits NSCLC tumor growth in vivo. Mol Cancer Ther. 2015 Sep;14(9):2014-22.


    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?