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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

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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

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 public 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