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UNC2250 Mertk inhibitor

Name: UNC2250
Brand: Selleck Chemicals
SKU: S7342
Availability: InStock
Rating: 5 (16 reviews)

Cat.No.S7342

UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

Chemical Structure

Molecular Weight: 440.58

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S734201 DMSO]2 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.43%

99.43

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	UNC2881 MRX-2843 UNC2541 UNC5293

Chemical Information, Storage & Stability

Molecular Weight	440.58	Formula	C₂₄H₃₆N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1493694-70-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCCNC1=NC=C(C(=N1)NC2CCC(CC2)O)C3=NC=C(C=C3)CN4CCOCC4

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (4.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.	0.130mg/ml (0.30mM)	Taking the 1 mL working solution as an example, add 50 μL 2.5 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to make it clear. Volume up to 1 mL. 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.

Mechanism of Action

Targets/IC₅₀/Ki	Mer ^[1] 1.7 nM Tyro3 ^[1] 100 nM
In vitro	UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, this compound also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells. ^[1]
Kinase Assay	Microfluidic Capillary Electrophoresis (MCE) Assay
Kinase Assay	Activity assays are performed in a 384-well, polypropylene microplate in a final volume of 50 μL of 50 mM Hepes, pH 7.4, containing 10 mM MgCl₂, 1.0 mM DTT, 0.01% Triton X-100, 0.1% bovine serum albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions are terminated by addition of 20 μL of 70 mM EDTA. After an 180 min incubation, phosphorylated and unphosphorylated substrate peptides are separated in buffer supplemented with 1× CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data are analyzed using EZ Reader software.
In vivo	According to in vivo PK experiment, UNC2250 has a moderate half-life, clearance, and volume of distribution as well as reasonable oral bioavailability and good solubility. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/24195762/

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