Danusertib

Danusertib : Inhibitor of AURKA, AURKB, AURKC

Structure

SERP Rating

Probe Danusertib is in the process of SERP review.

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Information

AURKA
AURKB
AURKC

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: Ki

Potency Value: 2.5 nM

Potency Assay: Biochemical Assay

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

Target aliases:

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

DOI Reference: 10.1021/jm060897w

Uniprot ID: O14965

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 13 nM

Potency Assay: Biochemical Assay

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

Target aliases:

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

DOI Reference: 10.1021/jm060897w

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Danusertib inhibits an additional set of protein kinases, namely, ABL, RET, TRKA, and FGFR1 in the nanomolar range. IC50s in uM: Aurora-A 0.013, VEGFR3 0.16 Aurora-B 0.079, C-KIT 0.407 Aurora-C 0.061, VEGFR2 0.432 ABL 0.025, CDK2/cyA 0.462 TRKA 0.030, STLK2 0.621 RET 0.031, FLT3 0.669 FGFR1 0.047, PLK1 3.5 LCK 0.155, others >10

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SERP ratings and comments

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