UNC2250

Catalog No.S7342

UNC2250 Chemical Structure

Molecular Weight(MW): 440.58

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.

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USD 570 In stock
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Cited by 4 Publications

2 Customer Reviews

  • UNC2250 induced suppression of MerTK-dependent signaling pathways in a dose-dependent manner. Z-138, Mino, and JVM-2 cells were treated with indicated concentrations of UNC2250 for 60 min; then, whole cell lysates were detected by western blot for phospholated and total MerTK, AKT, and p38.

    J Hematol Oncol, 2018, 11(1):43. UNC2250 purchased from Selleck.

    a-c Concentration of secreted IL-1β, IL-8 and CCL2 in THP-1 macrophages treated with or without recombinant human IL-37 (rhIL-37) for 3 h, followed by incubation for 1 h with or without Mertk inhibitor and then incubated with lipopolysaccharide (LPS) or MSU separately for a further 18 h; *P < 0.05. d Different dosage of rhIL-37 was given preventively or therapeutically with or without Mertk inhibitor intervention in mice with gouty arthritis, and foot thickness was evaluated; *P < 0.05. e, f Histopathological analysis by H&E staining in a joint from the group treated with rhIL-37 treatment and Mertk inhibitor intervention (×100 original magnification (e) and × 200 original magnification (f); arrow inflammation in soft tissue and joint space.

    Arthritis Res Ther, 2016, 18(1):268. UNC2250 purchased from Selleck.

Purity & Quality Control

Choose Selective TAM Receptor Inhibitors

Biological Activity

Description 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.
Targets
Mer [1]
()
Tyro3 [1]
1.7 nM 100 nM
In vitro

UNC2250 efficiently inhibits Mer phosphorylation in 697 B-ALL cells and Colo699 NSCLC cells. Moreover, UNC2250 also displays functional antitumor activity by reducing colony-forming potential in both rhabdoid tumor cells and NSCLC cells. [1]

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]

Protocol

Kinase Assay:[1]
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Microfluidic Capillary Electrophoresis (MCE) 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.
Cell Research:[1]
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  • Cell lines: BT-12 rhabdoid tumor cells, and Colo699 NSCLC cells
  • Concentrations: ~3 μM for BT-12, ~300 nM for Colo699
  • Incubation Time: 3 weeks for BT-12, 2 weeks for Colo699
  • Method: BT-12 rhabdoid tumor cells (10 000 cells) are cultured in 2.0 mL of 0.35% soft agar containing 0.5× RPMI medium, 7.5% FBS, and the indicated concentrations of 10 or DMSO vehicle only and overlaid with 0.5 mL of 1× RPMI medium containing 15% FBS and 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 2 times per week. Colonies were stained with thiazolyl blue tetrazolium bromide and counted after 3 weeks. Colo699 NSCLC cells (15 000 cells) are cultured in 1.5 mL of 0.35% soft agar containing 1× RPMI medium and 10% FBS and overlaid with 2.0 mL of 1× RPMI medium containing 10% FBS and the indicated concentrations of 10 or DMSO vehicle only. Medium and 10 or vehicle are refreshed 3 times per week. Colonies are stained with nitrotetrazolium blue chloride and counted after 2 weeks.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 2 mg/mL warmed (4.53 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
0.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 440.58
Formula

C24H36N6O2

CAS No. 1493694-70-4
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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TAM Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID