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RG7112 | RG7112 : 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
  • IC50:0.018 uM
  • IC50:0.4 uM
Antagonist
Up to 1 uM

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

In Vivo Validations

Nude mouse
Dose: 50 mg/kg
Route of delivery: Oral
Plasma half life: 8.8 h
Organ of interest (O): Subcutaneous xenografts (GBM and osteosarcoma), Brain engraftment (GBM)
Target engagement assay: In subcutaneous GBM xenografts, RG7112 increase expression of MDM2, p53 and p21.

Reference: --

Orthogonal Probes def

RO5353
AMG232
AM-6761

Chemical Information

Molecular Formula C38H48Cl2N4O4S
SMILEs CCOc1cc(C(C)(C)C)ccc1C1=N[C@@](C)(c2ccc(Cl)cc2)[C@@](C)(c2ccc(Cl)cc2)N1C(=O)N1CCN(CCCS(C)(=O)=O)CC1
InChI InChI=1S/C38H48Cl2N4O4S/c1-8-48-33-26-29(36(2,3)4)14-19-32(33)34-41-37(5,27-10-15-30(39)16-11-27)38(6,28-12-17-31(40)18-13-28)44(34)35(45)43-23-21-42(22-24-43)20-9-25-49(7,46)47/h10-19,26H,8-9,20-25H2,1-7H3/t37-,38+/m0/s1
Molecular weight 726.28 Da
AlogP 7.7549
HBond acceptors 8
HBond donors --
Atoms 97

References

Publications

    Cross References

    canSARChEMBLBindingDBPDBe (Protein Data Bank Europe)

    Vendors

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    Expert Reviews

    by SERP
    (on 7 Jun 2017 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP
    (on 28 Jun 2017 )
    Cellular Use Rating
    In Model Organisms
    Public notes can be found at http://www.citeulike.org/user/cdsouthan/article/14369611. Note it will also go live in the Guide to Pharmacology by August 2017 (Ligand 9699). Configuration of the...
    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