Home Protein Tyrosine Kinase FLT3 inhibitor - Mertk inhibitor - Axl inhibitor - Trk receptor inhibitor - Tyro3 inhibitor - c-Kit inhibitor - c-Met inhibitor UNC2025 For research use only.

UNC2025

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

UNC2025 Chemical Structure

CAS: 1429881-91-3

Selleck's UNC2025 has been cited by 5 publications

Purity & Quality Control

Batch: S966201 DMSO] 100 mg/mL] false] Ethanol] 60 mg/mL] false] Water] Insoluble] false Purity: 99.96%
99.96

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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)		 Click to View More Targets
0.35 nM 0.46 nM 1.65 nM 1.67 nM 4.38 nM
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models NOD/SCID/gamma mice
Dosages 3 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 476.66 Formula

C28H40N6O
CAS No. 1429881-91-3 SDF --
Smiles CCCCNC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4=CC=C(C=C4)CN5CCN(CC5)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (209.79 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble


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In vivo
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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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