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QP73 | QP73 : Degrader (PROTAC) of FTO
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FTO
  • IC50:1790 nM
  • DC50:34.9 nM
  • IC50:22.4 nM
  • Dmax:91%
  • DC50:65.9 nM
Degrader (PROTAC)
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Quantitative proteomic analysis was performed on NB4 cells treated with 300 nM QP73 and found FTO wa ...

Potency
Cellular
In Vitro

FTO

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.apsb.2024.07.016

In Vivo Validations

Mouse
Dose: 3 mg/kg
Route of delivery: Intravenous
Plasma half life: 1.25 ± 0.07 h
Systemic clearance: 20.1 ± 3.9 mL/min/kg)
Cmax: 2996 ± 441 ng/mL
Area Under the Curve:: 2532 ± 445 h × ng/mL

DOI Reference: 10.1016/j.apsb.2024.07.016

Dose: 5 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 0.50 h
Systemic clearance: 7.39 mL/min/Kg
Cmax: 578 ng/mL
Area Under the Curve:: 3201 h*ng/mL

DOI Reference: 10.1016/j.apsb.2024.07.016

Dose: 30 mg/kg
Route of delivery: Oral
Plasma half life: 0.50 h
Systemic clearance: 4.55 mL/min/Kg
Cmax: 49.1 ng/mL
Area Under the Curve:: 200 h*ng/mL

DOI Reference: 10.1016/j.apsb.2024.07.016

Negative Control Compounds

canSAR7437543
Notes: NB4 cells were treated with QP73N for 48 h did not show any degradation. Effect of QP73N on cell viability in NB4 and MV4-11 cells showed the compound is not toxic.

Chemical Information

Molecular Formula C39H36ClFN6O6
SMILEs Cc1noc(C)c1-c1cc(F)c(Nc2ccccc2C(=O)N2CCC3(CC2)CC(Nc2ccc4c(c2)C(=O)N(C2CCC(=O)NC2=O)C4=O)C3)c(Cl)c1
InChI InChI=1S/C39H36ClFN6O6/c1-20-33(21(2)53-45-20)22-15-28(40)34(29(41)16-22)43-30-6-4-3-5-26(30)36(50)46-13-11-39(12-14-46)18-24(19-39)42-23-7-8-25-27(17-23)38(52)47(37(25)51)31-9-10-32(48)44-35(31)49/h3-8,15-17,24,31,42-43H,9-14,18-19H2,1-2H3,(H,44,48,49)
Molecular weight 738.24 Da
AlogP 6.392640000000006
HBond acceptors 12
HBond donors 3
Atoms 89

References

Publications

Cross References

Expert Reviews

by SERP
(on 13 Feb 2025 )
Cellular Use Rating
In Model Organisms
Relevant signaling pathways are identified but off-target effects of the FTO PROTAC degrader QP73 on other m6A modifying proteins and broader profiling outside target family are lacking. A recent paper...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
In Model Organisms
The compound shows a clear time-dependent target degradation. However, selectivity profile has not been performed, so more data is needed despite proof of target engagement. The compound is well-characterised...
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