MK0457 is a pan-Aurora kinase inhibitor with a preference for Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM; Pollard & Mortimore; Harrington et al.) It is selective in a protein kinase screen (190 kinases tested) with the closest hit being Fms-related tyrosine kinase-3 (FLT-3; Ki = 30 nM; Pollard & Mortimore; Harrington et al.)
Inhibits proliferation of a wide variety of tumor cell lines in vitro (Harrington et al.; Li et al.; Arlot-Bonnemains et al.)
Blocks the growth of tumors in xenograft models of cancer, inhibits histone H3 phosphorylation, and increases apoptosis (Harrington et al.; Li et al.; Lin et al.)
Disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase (Li et al.)
Caractéristiques techniques
Marque
STEMCELL Technologies
Réf. B-LABO
BL-RE-126731
Réf. fabricant
17100202
CAS
639089-54-6
Synonyme
Tozasertib; VX 680
Quantité
50 mg
Formule moléculaire
C<sub>23</sub>H<sub>28</sub>N<sub>8</sub>OS
Pureté
≥98%
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