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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

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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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