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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
  • IC50:0.007 uM
Antagonist
--

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

In Vivo Validations

Male C57 mice, Female nude mice
Dose: 10 mg/kg (oral)
Route of delivery: Oral
Organ of interest (O): SJSA-1 xenografts (nude mice, 3-20 mg/kg)

Reference: --

Orthogonal Probes def

AMG232
AM-6761
MI-77301

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 5.6905
HBond acceptors 8
HBond donors 5
Atoms 70

References

Publications

    Cross References

    canSARChEMBLBindingDBPDBe (Protein Data Bank Europe)

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    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...
    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