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FMF-03-145-1 | FMF-03-145-1 : Inhibitor of AURKA, AURKB, AURKC
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
  • IC50:52 nM
  • EC50:38 nM
  • Inhibition:500 nM
AURKB
  • IC50:41 nM
  • EC50:11 nM
AURKC
  • IC50:53 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
PLK4

Gene ID: O00444

Organism: Homo sapiens

Family: Ser/Thr protein kinase family

Potency: IC50 - 82 nM

Potency Assay Off-Target:
Exclusively on-target activity detected by KINOMEscan ® at 1 μ M compound concentration with only on ...

Potency
Cellular
In Vitro

AURKA

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2017.08.016

AURKB

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2017.08.016

AURKC

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2017.08.016

Chemical Information

Molecular Formula C30H29N7O3
SMILEs CCC(=O)Nc1ccc(C(=O)Nc2ccc(Nc3ncc4c(n3)N(C)c3ccc(C)cc3C(=O)N4C)cc2)cc1
InChI InChI=1S/C30H29N7O3/c1-5-26(38)32-20-9-7-19(8-10-20)28(39)33-21-11-13-22(14-12-21)34-30-31-17-25-27(35-30)36(3)24-15-6-18(2)16-23(24)29(40)37(25)4/h6-17H,5H2,1-4H3,(H,32,38)(H,33,39)(H,31,34,35)
Molecular weight 535.23 Da
AlogP 5.48732
HBond acceptors 10
HBond donors 3
Atoms 69

Vendors

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Expert Reviews

by SERP
(on 23 Dec 2022 )
Cellular Use Rating
An orthogonal PLK4 inhibitor should be used in parallel to rule out phenotypic effects that result from PLK4 inhibition.
by SERP
(on 3 Jan 2023 )
Cellular Use Rating
A great addition to known AURK inhibitors and worth using in cells for this family of kinases. With several AURK probes and inhibitors available, this should be used in combination with other structurally...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
Considering that FMF-03-145-1 addresses the off-target PLK4 with an in vitro IC50 of 82 nM, which is comparable to the IC50 of the aurora kinases, an additional AURK probe with a different selectivity...
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