UNC2025

For research use only.

Catalog No.S9662

2 publications

UNC2025 Chemical Structure

CAS No. 1429881-91-3

UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 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.

Selleck's UNC2025 has been cited by 2 publications

Purity & Quality Control

Choose Selective FLT3 Inhibitors

Biological Activity

Description UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 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.
Targets
FLT3 [1]
(Cell-free assay)
Mer [1]
(Cell-free assay)
Axl [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
TrkC [1]
(Cell-free assay)
0.35 nM 0.46 nM 1.65 nM 1.67 nM 4.38 nM
In vitro

Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.[1]

In vivo

UNC2025 is a potent and highly orally bioavailable Mer inhibitor that is capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: 697 B-ALL, A549 NSCLC, Molm-14 AML cell lines
  • Concentrations: 2 nM, 4 nM, 8 nM, 10 nM, 12 nM, 16 nM, 20 nM, 30 nM, 40 nM, 50 nM
  • Incubation Time: 1 h
  • Method:

    697 Cells are treated with the indicated concentrations of UNC2025 for 1 h. Pervanadate is added to cultures for 3 min to stabilize the phosphorylated form of Mer. Mer is immunoprecipitated from cell lysates, and total MER protein and Mer phosphoprotein (p-Mer) are detected by immunoblot.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NOD/SCID/gamma mice
  • Dosages: 3 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (209.79 mM)
Water Insoluble
Ethanol ''60 mg/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 476.66
Formula

C28H40N6O

CAS No. 1429881-91-3
Storage powder
in solvent
Synonyms N/A
Smiles CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C

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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

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FLT3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID