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AMG232 | AMG232 : Inhibitor of MDM2-p53 interaction
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
  • Kd:0.045 nM
  • IC50:0.6 nM
  • IC50:9.1 nM
  • IC50:10 nM
Inhibitor
10-100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
AMG232 showed minimal activity in CYP3A4-inhibition assay and PXR-induction assay.

Potency
Cellular
In Vitro

MDM2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm401753e

In Vivo Validations

Rat, Athymic, nude mice
Dose: 0.5 mg/kg (rat)
Route of delivery: Intravenous, Subcutaneous
Plasma half life: 2.4 h
Systemic clearance: 0.66 L/h/kg
Organ of interest (O): SJSA-1 xenograft
Target engagement assay: AMG232 dose-dependently increased p21 RNA in xenografts.

DOI Reference: 10.1021/jm401753e

Orthogonal Probes def

RO5353
SAR-405838
AM-6761

Chemical Information

Molecular Formula C28H35Cl2NO5S
SMILEs CC(C)[C@@H](CS(=O)(=O)C(C)C)N1C(=O)[C@@](C)(CC(=O)O)C[C@H](c2cccc(Cl)c2)[C@H]1c1ccc(Cl)cc1
InChI InChI=1S/C28H35Cl2NO5S/c1-17(2)24(16-37(35,36)18(3)4)31-26(19-9-11-21(29)12-10-19)23(20-7-6-8-22(30)13-20)14-28(5,27(31)34)15-25(32)33/h6-13,17-18,23-24,26H,14-16H2,1-5H3,(H,32,33)/t23-,24-,26-,28-/m1/s1
Molecular weight 567.16 Da
AlogP 6.3794
HBond acceptors 6
HBond donors 1
Atoms 72

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 24 Jul 2017 )
Cellular Use Rating
In Model Organisms
This is a potent, competitive inhibitor of the p53-MDM2 interaction. It has been demonstrated to interrupt p53 binding to MDM2 and induce death in SJSA-1 osteosarcoma cells in a p53-dependent manner....
by SERP
(on 28 Jul 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 11 Nov 2020 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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