1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. UNC2025

UNC2025 is a potent, ATP-competitive, highly orally active and BBB-permeable Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.

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No. CAS : 1429881-91-3

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10 mM * 1 mL in DMSO
ready for reconstitution
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Revisión del cliente

Based on 8 publication(s) in Google Scholar

Other Forms of UNC2025:

Top Publications Citing Use of Products

    UNC2025 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Mar 9;44(3):658-675.e12.  [Abstract]

    UNC2025 (2 μM) abolished the effect that LEPR+ KCs engulfed more AKP-pHrodo cells.

    UNC2025 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Mar 9;44(3):658-675.e12.  [Abstract]

    UNC2025 (10 mg/kg; i.p; once every 4 d) produced antitumor effects in mice with intact LEPR+ KCs, with tumor BLI signals similar to LRKC- DTR mice.

    UNC2025 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Mar 9;44(3):658-675.e12.  [Abstract]

    UNC2025 (10 mg/kg; i.p; once every 4 d) suppressed metastasis and prolonged survival of NSG mice with hKC reconstitution.

    UNC2025 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2026 Mar 24:62:669-685.  [Abstract]

    UNC2025 (10 nM) effectively inhibited MERTK protein expression in macrophages.

    UNC2025 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2026 Mar 24:62:669-685.  [Abstract]

    UNC2025 (10 nM; 4 h) markedly attenuated upregulated expression of MERTK and its downstream effector Arg 1 in BMDMs induced by G-ELNs.
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    Descripciòn

    UNC2025 is a potent, ATP-competitive, highly orally active and BBB-permeable Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia[1][2][3].

    IC50 & Target

    IC50: 0.74 nM (Mer); 0.8 nM (Flt3)[1]

    Cellular Effect
    Cell Line Type Value Description References
    697 IC50
    2.7 1
    Compound: UNC2025
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    [PMID: 32659083]
    697 IC50
    2.7 1
    Compound: UNC2025
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    [PMID: 32659083]
    697 IC50
    2.7 1
    Compound: 11, UNC2025
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    697 IC50
    2.7 1
    Compound: 11, UNC2025
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    MOLM-14 IC50
    14 1
    Compound: UNC2025
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    [PMID: 32659083]
    MOLM-14 IC50
    14 1
    Compound: 11, UNC2025
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    697 IC50
    2.7 1
    Compound: 11, UNC2025
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    MOLM-14 IC50
    14 1
    Compound: 11, UNC2025
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    697 IC50
    2.7 1
    Compound: UNC2025
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    Cytotoxicity activity against human 697 cells assessed as reduction cell viability at 50 uM incubated for 48 hrs by ATP-glo assay
    [PMID: 32659083]
    MOLM-14 IC50
    14 1
    Compound: UNC2025
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    [PMID: 32659083]
    MOLM-14 IC50
    14 1
    Compound: 11, UNC2025
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry
    [PMID: 25068800]
    MOLM-14 IC50
    14 1
    Compound: UNC2025
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    Cytotoxicity against human MOLM-14 cells assessed as reduction in cell viability incubated for 72 hrs
    [PMID: 32659083]
    In Vitro

    UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively[1].
    UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50 of 2.7 nM in 697 B-ALL cells[1].
    UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells[1].
    UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells[1].
    UNC2025 (14 nM-10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells[2].
    UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    Cell Line: 32D Cells
    Concentration: 0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
    Incubation Time: 1 hour
    Result: Inhibited p-MEK, p-AXL, p-TYRO3 expression

    Cell Viability Assay[2]

    Cell Line: Mononuclear cells 
    Concentration: 14 nM–10μM
    Incubation Time: 48 hour
    Result: Showed IC50 values ranged from 9.0 nM to >10μ M with a median IC50 of 2.38 μM.

    Western Blot Analysis[2]

    Cell Line: MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines
    Concentration: 25-300 nM
    Incubation Time: 1 hour
    Result: Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.
    In Vivo

    UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively[2].
    UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: NSG mice injected with 697 B-ALL cells[2]
    Dosage: 50 or 75 mg/kg
    Administration: Orally adminstration
    Result: Delayed the disease progression.
    Peso molecular

    476.66

    Fòrmula

    C28H40N6O

    No. CAS
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CN1CCN(CC2=CC=C(C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (209.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0979 mL 10.4897 mL 20.9793 mL
    5 mM 0.4196 mL 2.0979 mL 4.1959 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureza y Documentación
    Referencias

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0979 mL 10.4897 mL 20.9793 mL 52.4483 mL
    5 mM 0.4196 mL 2.0979 mL 4.1959 mL 10.4897 mL
    10 mM 0.2098 mL 1.0490 mL 2.0979 mL 5.2448 mL
    15 mM 0.1399 mL 0.6993 mL 1.3986 mL 3.4966 mL
    20 mM 0.1049 mL 0.5245 mL 1.0490 mL 2.6224 mL
    25 mM 0.0839 mL 0.4196 mL 0.8392 mL 2.0979 mL
    30 mM 0.0699 mL 0.3497 mL 0.6993 mL 1.7483 mL
    40 mM 0.0524 mL 0.2622 mL 0.5245 mL 1.3112 mL
    50 mM 0.0420 mL 0.2098 mL 0.4196 mL 1.0490 mL
    60 mM 0.0350 mL 0.1748 mL 0.3497 mL 0.8741 mL
    80 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6556 mL
    100 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5245 mL
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    Nombre del producto:
    UNC2025
    Cat. No.:
    HY-12344
    Cantidad:
    MCE Japan Authorized Agent: