UNC2025
Based on 9 publication(s) in Google Scholar
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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- Pureza: 99.92%
- No. CAS: 1429881-91-3
- Fòrmula: C28H40N6O
- Peso molecular:476.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Kinase Inhibitor Library
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Publications Citing Use of MedChemExpress (MCE) UNC2025
More- Cancer Cell. 2026 Mar 9;44(3):658-675.e12. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Bioact Mater. 2026 Mar 24:62:669-685. [Abstract]
- Research (Wash D C). 2025 Aug 25:8:0838. [Abstract]
- Fundam Res. 2024 Apr 15.
- Int J Mol Med. 2026 Apr;57(4):85. [Abstract]
- J Ethnopharmacol. 2024 Sep 15:331:118290. [Abstract]
- Oncol Rep. 2020 Oct;44(4):1322-1332. [Abstract]
- bioRxiv. 2026 Jun 26.
Customer Validation & Images
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Flow Cytometry
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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WB
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WB
Actividad biológica
IC50: 0.74 nM (Mer); 0.8 nM (Flt3)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
2.7 nM
Compound: 11, UNC2025
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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
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[PMID: 25068800] |
| 697 | IC50 |
2.7 nM
Compound: UNC2025
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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
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[PMID: 32659083] |
| MOLM-14 | IC50 |
14 nM
Compound: 11, UNC2025
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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
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[PMID: 25068800] |
| MOLM-14 | IC50 |
14 nM
Compound: UNC2025
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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
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[PMID: 32659083] |
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.
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Cell Line:32D Cells
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Concentration:0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
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Incubation Time:1 hour
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Result:Inhibited p-MEK, p-AXL, p-TYRO3 expression
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Cell Line:Mononuclear cells
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Concentration:14 nM–10μM
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Incubation Time:48 hour
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Result:Showed IC50 values ranged from 9.0 nM to >10μ M with a median IC50 of 2.38 μM.
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Cell Line:MERTK-expressing B-cell and T-cell acute lymphoid leukemia (B-ALL and T-ALL) and acute myeloid leukemia (AML) cell lines
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Concentration:25-300 nM
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Incubation Time:1 hour
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Result:Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice injected with 697 B-ALL cells[2]
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Dosage:50 or 75 mg/kg
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Administration:Orally adminstration
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Result:Delayed the disease progression.
Chemical Information
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No. CAS 1429881-91-3
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Appearance Solid
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Peso molecular 476.66
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Fòrmula C28H40N6O
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Color White to light yellow
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SMILES
CN1CCN(CC2=CC=C(C3=CN([C@@H]4CC[C@@H](O)CC4)C5=NC(NCCCC)=NC=C53)C=C2)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Chemotherapy triggers immune evasion by fostering LEPR+ Kupffer cell differentiation in liver metastases. [Abstract]2026 Mar 9;44(3):658-675.e12. PMID: 41687606
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.
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Bioact Mater
Activating the cellular scavenger: A bioactive hydrogel promotes diabetic wounds via plant exosome-like nanovesicles enhanced macrophage efferocytosis. [Abstract]2026 Mar 24:62:669-685. PMID: 41937946
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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Research (Wash D C)
Targeting the ANXA8-SP1-PPA1 Axis to Modulate TCA Cycle and Matrix Deposition in Diffuse-Type Gastric Cancer. [Abstract]2025 Aug 25:8:0838. PMID: 40862051 -
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Int J Mol Med
Hypothermic machine perfusion protects DCD graft liver from ischemia‑reperfusion injury by enhancing macrophage efferocytosis via KLF2‑NLRP3 signaling. [Abstract]2026 Apr;57(4):85. PMID: 41645764 -
J Ethnopharmacol
HuoXueTongFu formula induces M2c macrophages via the MerTK/PI3K/AKT pathway to eliminate NETs in intraperitoneal adhesion in mice. [Abstract]2024 Sep 15:331:118290. PMID: 38703872 -
Oncol Rep
Modulation of protein S and growth arrest specific 6 protein signaling inhibits pancreatic cancer cell survival and proliferation. [Abstract]2020 Oct;44(4):1322-1332. PMID: 32945517 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41. [Content Brief]
[2]. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. [Content Brief]
[3]. Wu J, et al. MerTK as a therapeutic target in glioblastoma. Neuro Oncol. 2018 Jan 10;20(1):92-102. [Content Brief]
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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