UNC2025 hydrochloride

Name: UNC2025 hydrochloride
Brand: MedChemExpress
SKU: HY-12344A
Rating: 5.0 (4 reviews)

Cat. No.: HY-12344A Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active 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; K_i = 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.

UNC2025 hydrochloride Chemical Structure

CAS No. : 2070015-17-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 68	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 68	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of UNC2025 hydrochloride:

UNC2025 In-stock

4 Publications Citing Use of MCE UNC2025 hydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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 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:	Oral adminstration
Result:	Delayed the disease progression.

Molecular Weight

513.12

Formula

C₂₈H₄₁ClN₆O

CAS No.

2070015-17-5

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
10 mM	0.1949 mL	0.9744 mL	1.9489 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)

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: ≥ 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)

Dosing volume
(per animal)

μL

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: 99.87%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (251 KB) RP-HPLC (204 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]

Complete Stock Solution Preparation Table

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.