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      UNC-2025
      UNC-2025

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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 #: 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.

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      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 


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      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.

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