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CC-90009 | CC-90009 : Molecular Glue, degrader of GSPT1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
GSPT1
  • DC50:9 nM
  • Dmax:88% @ 20 h
Molecular Glues
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
<strong>Proteomics:</strong> Proteomic experiments with concentration range from 0.20 μM up to 3 μ ...

Potency
Cellular
In Vitro

GSPT1

Mode of Action: Molecular Glues

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.0c01489

In Vivo Validations

Mouse, Rat, Cyno
Dose: 2 mg/Kg (M, R); 1 mg/Kg (Cyno)
Route of delivery: Intravenous
Plasma half life: 9.3 h
Systemic clearance: 67.9 (M), 28.3 (R), 6 (C) mL/min/kg
Volume of Distribution at Steady-State: Across all doses and schedules, volume of distribution was 61.69 L
Target engagement assay: Efficacy studies in J. Med. Chem. 2021, 64, 4, 1835–1843 utilise 2.5 mg/kg and 5mg/kg BID dosing.

DOI Reference: 10.1021/acs.jmedchem.0c01489

Orthogonal Probes def

MG-277

Chemical Information

Molecular Formula C22H18ClF2N3O4
SMILEs O=C1CCC(N2Cc3cc(CNC(=O)C(F)(F)c4ccc(Cl)cc4)ccc3C2=O)C(=O)N1
InChI InChI=1S/C22H18ClF2N3O4/c23-15-4-2-14(3-5-15)22(24,25)21(32)26-10-12-1-6-16-13(9-12)11-28(20(16)31)17-7-8-18(29)27-19(17)30/h1-6,9,17H,7-8,10-11H2,(H,26,32)(H,27,29,30)
Molecular weight 461.10 Da
AlogP 2.5092
HBond acceptors 7
HBond donors 2
Atoms 50

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 17 Dec 2021 )
Cellular Use Rating
In Model Organisms
CC-90009 is a potent, highly selective and thoroughly characterised molecule for investigating effects of GSPT1 degradation both in cells and a range of in vivo models.
by SERP
(on 20 Dec 2021 )
Cellular Use Rating
In Model Organisms
CC-90009 is a well-validated drug candidate that can also be used as a chemical probe to degrade GSPT1.
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