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AMG900 | AMG900 : ATP competitive inhibitor of AURKA, AURKB, AURKC
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
AURKA
  • IC 50:5 nM
  • IC 50:6.5-8.2 nM
AURKB
  • IC 50:4 nM
  • IC 50:6.5-8.2 nM
AURKC
  • IC 50:1 nM
  • IC50:6.5-8.2 nM
ATP competitive
Up to 100 nM

Selectivity

In Vitro Selectivity Assessment
MAPK14

Gene ID: Q16539

Organism: Homo sapiens

Family: CMGC Ser/Thr protein kinase family

Potency: IC 50 - 53 nM

Potency Assay Off-Target:
AMG900 was tested in enzyme inhibition assays and ATP-competitive binding assays (Ambit Biosciences) ...
Selectivity Assessment Description:
IC50s are from enzyme inhibition assays. In ATP-competitive binding assays, AMG900 had KD < 50 nM fo ...

Potency
Cellular
In Vitro

AURKA

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-10-3001

AURKB

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-10-3001

AURKC

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-10-3001

In Vivo Validations

Mouse
Dose: 3.75-15 mg/kg
Route of delivery: Oral
Organ of interest (O): xenograft, bone marrow
Target engagement assay: Indirect: in xenografts and bone marrow, AMG900 inhibited phosphorylation of substrates for Aurora kinases.

DOI Reference: 10.1158/0008-5472.CAN-10-3001

Orthogonal Probes def

MK-5108
XMD-12
AZD1152

Chemical Information

Molecular Formula C28H21N7OS
SMILEs Cc1csc(-c2nnc(Nc3ccc(Oc4ncccc4-c4ccnc(N)n4)cc3)c3ccccc23)c1
InChI InChI=1S/C28H21N7OS/c1-17-15-24(37-16-17)25-20-5-2-3-6-21(20)26(35-34-25)32-18-8-10-19(11-9-18)36-27-22(7-4-13-30-27)23-12-14-31-28(29)33-23/h2-16H,1H3,(H,32,35)(H2,29,31,33)
Molecular weight 503.15 Da
AlogP 6.63682
HBond acceptors 8
HBond donors 3
Atoms 58

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 29 May 2016 )
Cellular Use Rating
In Model Organisms
AMG900 is an orally available, small molecule, ATP-competitive, low single-digit nM, pan-Aurora-kinase inhibitor (AKI). It shows at least 10-fold in vitro selectivity compared with relevant Janus kinase...
by SERP
(on 31 May 2016 )
Cellular Use Rating
In Model Organisms
AMG900 is a potent pan Aurora inhibitor that is active in tumor cell lines irrespective of P-gp or BCRP status. Compound is orally bioavailable in mice, rats, dogs and monkeys.
by SERP
(on 26 Dec 2016 )
Cellular Use Rating
In Model Organisms
AMG900 is a potent ATP-competitive inhibitor of Aurora kinases. It exhibits low nanomolar affinity for Aurora kinases (A, B, and C); it also has low nanomolar affinity for DDR1, 10-100 nanomolar affinity...
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