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RO2468 | Antagonist of MDM2
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
MDM2
  • IC50:6 nM
  • IC50:150 nM
up to 1 uM

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/ml400359z

In Vivo Validations

Mouse
Dose: 10 mg/Kg QD
Route of delivery: Intravenous, Oral
Plasma half life: 3 h (IV)
Systemic clearance: 1,8 mL/min/kg (IV)
Organ of interest (O): SJSA-1 xenografts (nude mice, 3-20 mg/kg)

DOI Reference: 10.1021/ml400359z

Orthogonal Probes def

NAVTEMADLIN
MD-4251

Chemical Information

Molecular Formula C30H30Cl2FN5O4
SMILEs COc1cc(C(N)=O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@@]2(C(=O)Nc3cc(Cl)ncc32)[C@H]1c1cccc(Cl)c1F
InChI InChI=1S/C30H30Cl2FN5O4/c1-29(2,3)12-21-30(16-13-35-22(32)11-19(16)37-28(30)41)23(15-6-5-7-17(31)24(15)33)25(38-21)27(40)36-18-9-8-14(26(34)39)10-20(18)42-4/h5-11,13,21,23,25,38H,12H2,1-4H3,(H2,34,39)(H,36,40)(H,37,41)/t21-,23-,25+,30+/m0/s1
Molecular weight 613.17 Da
AlogP 5.024000000000004
HBond acceptors 9
HBond donors 5
Atoms 72

Vendors

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Expert Reviews

by SERP
(on 29 Apr 2020)
Cellular Use Rating
In Model Organisms
This is an excellent chemical probe and although the selectivity data is lacking, the biological effect in p53 WT vs MUT cell lines looks convincing (over 700 fold difference in IC50s). Still, I would...
by SERP
(on 16 May 2020)
Cellular Use Rating
In Model Organisms
This is overall an excellent chemical probe against MDM2, based on in vitro biochemical binding affinity, cellular activity and selectivity, and an impressive in vivo/xenografts...
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