ALISERTIB

ALISERTIB : Inhibitor of AURKA

Structure

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Information

AURKA

Inhibitor

up to 100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 3.5 nM

Potency Assay: Radiometric assays containing 100 μM [γ-32P] ATP and quantified by p81 phosphocellulose assay and scintillation counting

PDB ID for probe-target interaction (3D structure): 5IA0

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

DOI Reference: 10.1021/cb100053q

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 1.2 nM

Potency Assay: Assayed using recombinant protein

PDB ID for probe-target interaction (3D structure): 5IA0

Target aliases:

Aurora kinase A, STK6, STK15, IAK1, BTAK, AYK1, AU ...

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

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Alisertib has less activity against AURKB, with an IC50 value of 396.5 nM and showed selectivity in enzymatic assays against a 205-kinase panel at a concentration of 1 μM.

Potency assay, off target (cells): In HeLa cells, Alisertib is very selective against AURKB (IC50 = 1,534 nM)

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