UNC2025

Name: UNC2025
Brand: MedChemExpress
SKU: HY-12344
Rating: 5.0 (8 reviews)

Cat. No.: HY-12344 Purity: 99.92%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

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.

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

CAS No. : 1429881-91-3

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of UNC2025:

UNC2025 hydrochloride In-stock

8 Publications Citing Use of MCE UNC2025

Flow Cytometry

In Vivo Efficacy Study

: UNC2025 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 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 LR^{KC- DTR} mice.

: UNC2025 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 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 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.

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References
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Description

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.

Molecular Weight

476.66

Formula

C₂₈H₄₀N₆O

CAS No.

1429881-91-3

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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
10 mM	0.2098 mL	1.0490 mL	2.0979 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) HNMR (192 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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

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

UNC2025 Related Classifications

Help & FAQs

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.

Keywords:

UNC20251429881-91-3UNC 2025UNC-2025FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3acuteleukemiaMERTKcancerInhibitorinhibitorinhibit

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UNC2025

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UNC2025 Related Antibodies

8 Publications Citing Use of MCE UNC2025

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