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    UNC-2025 HCl
    UNC-2025 HCl

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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 #: V0586
    CAS #: 1429881-91-3 (free base)Purity ≥98%

    Description: UNC-2025 HCl (known also as UNC2025), the Hydrochloride salt of UNC-2025, is an orally bioavailable and selective MER/FLT3 dual inhibitor with potential antineoplastic activity. It inhibits MER/FLT3 kinases with IC50s of 0.74 nM and 0.8 nM, respectively. UNC 2025 displayed about 20-fold selectivity for inhibiting MER/FLT3 over Axl and Tyro3. UNC-2025 is also capable of inhibiting Mer phosphorylation in vivo and shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy.

    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)513.12
    FormulaC28H41ClN6O
    CAS No.1429881-91-3 (free base)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 25 mg/mL (48.7 mM)
    Water: 100 mg/mL (194.9 mM)
    Ethanol: 8 mg/mL (15.6 mM)
    SMILESCN1CCN(CC2=CC=C(C3=CN([[email protected]@H]4CC[[email protected]@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1.[H]Cl
    SynonymsUNC-2025 HCl; UNC-2025 hydrochloride; UNC2025 hydrochloride; UNC 2025 HCl; UNC2025 HCl; UNC 2025 hydrochloride; UNC-2025, UNC2025, UNC 2025


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    In Vitro

    In vitro activity: 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.


    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. 


    Cell Assay: 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 HCl

    UNC2025 Inhibits Signaling Pathways Downstream of MERTK. Mol Cancer Ther. 2015 Sep; 14(9): 2014–2022.

    UNC-2025 HCl

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


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