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ALISERTIB | ALISERTIB : Inhibitor of AURKA
RATINGS:
Cellular Use: (0 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
  • IC50:3.5 nM
  • IC50:1.2 nM
  • IC50:6.7 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Alisertib has less activity against AURKB, with an IC50 value of 396.5 nM and showed selectivity in ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In HeLa cells, Alisertib is very selective against AURKB (IC50 = 1,534 nM)

Potency
Cellular
In Vitro

AURKA

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/cb100053q

In Vivo Validations

Mouse
Dose: 5, 10, 30 mg/Kg
Route of delivery: Oral
Target engagement assay: Alisertib treatment resulted in a dose-dependent TGI of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups, respectively

DOI Reference: 10.1158/1078-0432.CCR-11-1536

Orthogonal Probes def

AMG-900
MK-5108

Chemical Information

Molecular Formula C27H20ClFN4O4
SMILEs COc1cc(Nc2ncc3c(n2)-c2ccc(Cl)cc2C(c2c(F)cccc2OC)=NC3)ccc1C(=O)O
InChI InChI=1S/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33)
Molecular weight 518.12 Da
AlogP 5.7461
HBond acceptors 8
HBond donors 2
Atoms 57

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Expert Reviews

No SERP comments found for ALISERTIB

Probe ALISERTIB is in the process of SERP review.

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