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

UNC2025 hydrochloride 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 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.

For research use only. We do not sell to patients.

CAS No. : 2070015-17-5

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of UNC2025 hydrochloride:

Top Publications Citing Use of Products

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

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

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

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

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

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

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

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

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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    UNC2025 hydrochloride 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 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia[1].

    IC50 & Target

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

    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 Proliferation Assay[1]

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

    Western Blot Analysis[2]

    Cell Line: Kasumi-1 AML and 697 B-ALL cells
    Concentration: 25-300 nM
    Incubation Time: 48 hours
    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: Oral adminstration
    Result: Delayed the disease progression.
    Molecular Weight

    513.12

    Formula

    C28H41ClN6O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    H2O : 55 mg/mL (107.19 mM; Need ultrasonic)

    DMSO : 10 mg/mL (19.49 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 1.9489 mL 9.7443 mL 19.4886 mL
    5 mM 0.3898 mL 1.9489 mL 3.8977 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 1 mg/mL (1.95 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.95 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 100 mg/mL (194.89 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.96%

    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.9489 mL 9.7443 mL 19.4886 mL 48.7215 mL
    5 mM 0.3898 mL 1.9489 mL 3.8977 mL 9.7443 mL
    10 mM 0.1949 mL 0.9744 mL 1.9489 mL 4.8722 mL
    15 mM 0.1299 mL 0.6496 mL 1.2992 mL 3.2481 mL
    H2O 20 mM 0.0974 mL 0.4872 mL 0.9744 mL 2.4361 mL
    25 mM 0.0780 mL 0.3898 mL 0.7795 mL 1.9489 mL
    30 mM 0.0650 mL 0.3248 mL 0.6496 mL 1.6241 mL
    40 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.2180 mL
    50 mM 0.0390 mL 0.1949 mL 0.3898 mL 0.9744 mL
    60 mM 0.0325 mL 0.1624 mL 0.3248 mL 0.8120 mL
    80 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6090 mL
    100 mM 0.0195 mL 0.0974 mL 0.1949 mL 0.4872 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    UNC2025 hydrochloride
    Cat. No.:
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