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RG7388 | Antagonist of MDM2
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
MDM2
  • IC50:6 nM
  • Kd:9.79 nM
  • IC50:30 nM
Antagonist
10-500 nM

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm400487c

In Vivo Validations

Mouse
Dose: 50 mg/kg (oral); 5 mg/kg (IV)
Route of delivery: Intravenous, Oral
Plasma half life: 1.6 h (IV)
Systemic clearance: 10.3 mL/mg/kg (IV)
Organ of interest (O): SJSA1 tumor xenograft
Target engagement assay: Indirect, inhibition of tumor growth.

DOI Reference: 10.1021/jm400487c

Orthogonal Probes def

RO5353
AM-6761
AMG232

Chemical Information

Molecular Formula C31H29Cl2F2N3O4
SMILEs COc1cc(C(=O)O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F
InChI InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31-/m0/s1
Molecular weight 615.15 Da
AlogP 6.93888
HBond acceptors 7
HBond donors 3
Atoms 71

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 17 Aug 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 17 Aug 2017 )
Cellular Use Rating
In Model Organisms
RG7388 is a second-generation inhibitor of the protein-protein interaction that occurs between wild type p53 (a potent tumor suppressor) and the E3 ubiquitin ligase MDM2. High levels of MDM2 are found...
by SERP
(on 16 Nov 2020 )
Cellular Use Rating
In Model Organisms
Potent and optimised MDM2-p53 antagonist that entered into clinical trials. In general, there is only very limited data available with regard to the selectivity of this compound. However, in contrast...
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