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UNC2025 | UNC2025 : ATP-competitive inhibitor of FLT3, MERTK
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FLT3
  • IC 50:0.8 nM
  • IC 50:14 nM
MERTK
  • IC 50:0.74 nM
  • IC 50:2.7 nM
ATP competitive
1-20 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - AXL: 14 nM, TYRO3: 17 nM

Potency Assay Off-Target:
UNC2025 was tested against 305 kinases in microcapillary assay (Carna Biosciences). At 100 nM (>100- ...
Selectivity Assessment Description:
UNC2025 was tested against 305 kinases in microcapillary assay (Carna Biosciences). At 100 nM (>100- ...
In Cell Selectivity Assessment

Potency: IC50 - AXL: 122 nM, TYRO3: 301 nM

Potency Assay Off-Target:
In EGF-induced assays in 32D cells expressing EGFR-AXL or EGFR-TYRO3 fusion proteins, UNC2025 inhibi ...
Selectivity Assessment Description:
In EGF-induced assays in 32D cells expressing EGFR-AXL or EGFR-TYRO3 fusion proteins, UNC2025 inhibi ...

Potency
Cellular
In Vitro

FLT3

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm500749d

MERTK

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm500749d

In Vivo Validations

Mouse
Dose: 3 mg/mL
Route of delivery: Intravenous, Oral
Plasma half life: 3.8 h (IV)
Systemic clearance: 9.2 mg/mL/kg (IV)
Organ of interest (O): human bone marrow leukemia cell xenograft
Target engagement assay: UNC2025 dose-dependently inhibited MER phosphorylation.

DOI Reference: 10.1021/jm500749d

Negative Control Compounds

Compound 20 from J Med Chem paper

Chemical Information

Molecular Formula C28H40N6O
SMILEs CCCCNc1ncc2c(-c3ccc(CN4CCN(C)CC4)cc3)cn([C@H]3CC[C@H](O)CC3)c2n1
InChI InChI=1S/C28H40N6O/c1-3-4-13-29-28-30-18-25-26(20-34(27(25)31-28)23-9-11-24(35)12-10-23)22-7-5-21(6-8-22)19-33-16-14-32(2)15-17-33/h5-8,18,20,23-24,35H,3-4,9-17,19H2,1-2H3,(H,29,30,31)/t23-,24-
Molecular weight 476.33 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 75
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

by SERP
(on 17 Apr 2017 )
Cellular Use Rating
In Model Organisms
UNC2025 is a dual inhibitor of MER and FLT3 tyrosine kinases with a subnanomolar potency in a cell-free kinase assay (0.74 nM for MER and 0.80 nM for FLT3) and a low nanomolar-range potency in cell-based...
by SERP
(on 27 Apr 2017 )
Cellular Use Rating
In Model Organisms
UNC2025 is a dual inhibitor of MER and FLT3. In practice, it will not be feasible to distinguish MER from FLT3 effects for analyzing downstream pathways, although there seems several-fold difference...
by SERP
(on 16 May 2017 )
Cellular Use Rating
In Model Organisms
UNC2025 is a very well characterized, dual inhibitor of MER and FLT3 kinases with subnanomolar potency in vitro and low nanomolar potency in cells (2.7 nM for MER and 14 nM for FLT3). In this range,...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria