UNC5293

Name: UNC5293
Brand: TargetMol
SKU: T9134
Rating: 4.5 (1 reviews)

😃Good

Catalog No. T9134Cas No. 2226789-82-6

UNC5293 is a potent, orally available and highly MERTK-selective inhibitor with Ki of 190 pM. UNC5293 inhibits MERTK ( IC 50 =0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research [1].

UNC5293

😃Good

Catalog No. T9134Cas No. 2226789-82-6

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
25 mg	$1,650	8-10 weeks	8-10 weeks
50 mg	$2,150	8-10 weeks	8-10 weeks

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Resource Download

Product Introduction

Bioactivity

Description	UNC5293 is a potent, orally available and highly MERTK-selective inhibitor with Ki of 190 pM. UNC5293 inhibits MERTK ( IC 50 =0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research [1].
In vitro	UNC5293 demonstrates selective inhibition of its target in cell-based assays, effectively inhibiting MERTK phosphorylation in human B-cell acute lymphoblastic leukemia (B-ALL) cultures with an IC50 of 9.4 nM. However, it shows weaker activity against FLT3 in the SEM B-ALL cell line, with an IC50 of 170 nM [1].
In vivo	UNC5293 administered orally at a dosage of 120 mg/kg as a single dose significantly inhibits MERTK in vivo within orthotopic 697 B-ALL mouse xenograft models [1]. At a lower dosage of 3 mg/kg via oral gavage, UNC5293 demonstrates favorable pharmacokinetic attributes in mice, including a half-life of 7.8 hours, 58% oral bioavailability, a maximum concentration (C max) of 9.2 μM, and an area under the curve (AUC) of 2.5 h*μM [1].

Chemical Properties

Molecular Weight	518.69
Formula	C₃₀H₄₂N₆O₂
Cas No.	2226789-82-6
Smiles	CCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)C1CCN(CC1)C(=O)c1cc(C)nc(C)c1
Relative Density.	1.28 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc