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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

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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 public comments)
by SERP
(on 11 Nov 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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