Name: UNC2025 HCl
Brand: Selleck Chemicals
SKU: S7576
Availability: InStock
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other Axl Inhibitors	Bemcentinib (R428) Dubermatinib(TP-0903) LDC1267 CEP-40783 (RXDX-106) SGI-7079 Tamnorzatinib (ONO-7475) RU-301 PF-07265807

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
32D cells	Function assay		1 h	Inhibition of EGFR extracellular/transmembrane domain-tagged Mer intracellular domain (unknown origin) expressed in 32D cells assessed as inhibition EGF-stimulated of phosphorylation pretreated for 1 hr prior to EGF stimulation by Western blot analysis, IC50=2.7 nM
697 cells	Function assay		1 h	Inhibition of Mer phosphorylation in human 697 cells preincubated for 1 hr by densitometry, IC50=2.7 nM
Molm-14 cells	Function assay		1 h	Inhibition of Flt3 phosphorylation in human Molm-14 cells preincubated for 1 hr by densitometry, IC50=0.014 μM
A549 cells	Function assay	50-300 nM		Inhibition of Mer-mediated colony formation in human A549 cells at 50 to 300 nM measured after 2 weeks by soft agar colony formation assay
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (194.88 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.310mg/ml (0.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	513.12	Formula	C₂₈H₄₁ClN₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2070015-17-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UNC2025 hydrochloride			Smiles	CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Mer (Cell-free assay) 0.74 nM FLT3 (Cell-free assay) 0.8 nM Axl (Cell-free assay) 14 nM Tyro3 (Cell-free assay) 17 nM
In vitro	In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation.
In vivo	In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25068800/ [2] https://pubmed.ncbi.nlm.nih.gov/26162689/

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Handling Instructions

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UNC2025 HCl Axl inhibitor

Chemical Structure

Molecular Weight: 513.12