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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

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Targets Biochemical/Biophysical Potency Cellular Potency
MDM2
  • IC50:18 nM
  • IC50:400 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/ml4000657

In Vivo Validations

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.

DOI Reference: 10.1021/ml4000657

Orthogonal Probes def

AM-6761
NAVTEMADLIN
MD-4251

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 7.754900000000013
HBond acceptors 8
HBond donors --
Atoms 97

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 public 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...
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