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AM-6761 | Antagonist of MDM2
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
  • IC50:0.1 nM 0% HS; 0.8 nM 15% HS
  • IC50:16 nM
Antagonist
20 nM - 1 uM

Selectivity

Potency
Cellular
In Vitro

MDM2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm401911v

In Vivo Validations

Mouse, Rat
Dose: 0.5 mg/Kg (IV), 5 mg/Kg (PO)
Route of delivery: Intravenous, Oral
Plasma half life: 3.2 (M), 4.4 (R) h (IV)
Systemic clearance: 0.15 (M), 0.23 (R) L/h/Kg (IV)
Organ of interest (O): SJSA-1 osteosarcoma xenograft model
Target engagement assay: ED50 = 11 mg/kg

Other Reference: SJSA-1

Orthogonal Probes def

RO5353
AMG232
MI-77301

Chemical Information

Molecular Formula C33H37Cl2FN2O5S2
SMILEs CC(C)(C)S(=O)(=O)C[C@H](C1CC1)N1C(=O)[C@@](C)(Cc2ncc(CC(=O)O)s2)C[C@H](c2cccc(Cl)c2)[C@H]1c1ccc(Cl)c(F)c1
InChI InChI=1S/C33H37Cl2FN2O5S2/c1-32(2,3)45(42,43)18-27(19-8-9-19)38-30(21-10-11-25(35)26(36)13-21)24(20-6-5-7-22(34)12-20)15-33(4,31(38)41)16-28-37-17-23(44-28)14-29(39)40/h5-7,10-13,17,19,24,27,30H,8-9,14-16,18H2,1-4H3,(H,39,40)/t24-,27-,30-,33-/m1/s1
Molecular weight 694.15 Da
AlogP 7.5142
HBond acceptors 7
HBond donors 1
Atoms 82

Vendors

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Expert Reviews

by SERP
(on 23 Jun 2017 )
Cellular Use Rating
In Model Organisms
AM-6761 is broadly comparable to the previously reported compound AMG-232 in terms of high potency and robust effects in cells. AM-6761 would be a confirmatory molecule from the same chemical scaffold....
by SERP
(on 27 Jun 2017 )
Cellular Use Rating
In Model Organisms
This is a good probe for cell and mouse studies, but it is probably less useful than related Amgen compounds that have entered human testing, such as AMG232. In a mouse xenograft SJSA-1 osteosarcoma...
by SERP
(on 6 Jul 2017 )
Cellular Use Rating
In Model Organisms
This is a high quality probe derived from AMG232 and broadly comparable to that clinical agent, with similar potency and in vivo anti-tumor activity in an SJSA-1 mouse model. Publications of AMG232...
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