UNC2025

Catalog No.S9662

For research use only.

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.

UNC2025 Chemical Structure

CAS No. 1429881-91-3

Selleck's UNC2025 has been cited by 3 Publications

Purity & Quality Control

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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)
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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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: NOD/SCID/gamma mice
  • Dosages: 3 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(209.79 mM)
Water Insoluble
Ethanol ''60 mg/mL

Chemical Information

Molecular Weight 476.66
Formula

C28H40N6O

CAS No. 1429881-91-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C

In vivo Formulation Calculator (Clear solution)

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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.
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Molarity Calculator

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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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