Art. -Nr.: HY-12344

UNC2025

9 Cited Publications

Kundenbewertung

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; K_i = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.92%
CAS. Nr.: 1429881-91-3
Formel: C₂₈H₄₀N₆O
Molecular Weight:476.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

UNC2025 Chemical Structure

CAS. Nr.: 1429881-91-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
697	IC₅₀	2.7 nM 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 nM 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 nM 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 nM 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 T_max, C_max, 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.

Chemical Information

CAS. Nr. 1429881-91-3
Appearance Solid
Molecular Weight 476.66
Formel C₂₈H₄₀N₆O
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

All Flow CytometryWBIn Vivo Efficacy Study

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Journal Impact Factor

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 LR^{KC- 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.
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.
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
Fundam Res

2024 Apr 15.
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
bioRxiv

2026 Jun 26.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0979 mL

10.4897 mL

20.9793 mL

5 mM

0.4196 mL

2.0979 mL

4.1959 mL

10 mM

0.2098 mL

1.0490 mL

2.0979 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

UNC2025

9 Cited Publications

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UNC2025

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC2025

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC2025

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Anti-Prostate Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC2025

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC2025 Related Classifications

Art. -Nr.: HY-12344