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RO5353 | 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
  • IC50:7 nM
  • IC50:7 nM
up to 100 nM

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 (oral)
Route of delivery: Oral
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 C29H29Cl2FN4O4S
SMILEs COc1cc(C(N)=O)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@@]2(C(=O)Nc3cc(Cl)sc32)[C@H]1c1cccc(Cl)c1F
InChI InChI=1S/C29H29Cl2FN4O4S/c1-28(2,3)12-19-29(24-17(35-27(29)39)11-20(31)41-24)21(14-6-5-7-15(30)22(14)32)23(36-19)26(38)34-16-9-8-13(25(33)37)10-18(16)40-4/h5-11,19,21,23,36H,12H2,1-4H3,(H2,33,37)(H,34,38)(H,35,39)/t19-,21-,23+,29+/m0/s1
Molecular weight 618.13 Da
AlogP 5.690500000000004
HBond acceptors 8
HBond donors 5
Atoms 70

Vendors

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Expert Reviews

by SERP
(on 27 Jul 2017)
Cellular Use Rating
In Model Organisms
RO5353 is an excellent probe to study the in vitro and in vivo biology of p53-MDM2 inhibition. It is potent, has excellent cellular selectivity and robust in-vivo efficacy at a dose (10 mg/kg) that...
by SERP
(on 28 Jul 2017)
Cellular Use Rating
In Model Organisms
RO5353 is potent against MDM2 (7 nM), showing equipotency (7 nM) in antiproliferative assays with multiple WT p53 cells lines (i.e., the expected on-target pharmacology). The average antiproliferative...
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