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Empesertib

Chemical Structure : Empesertib

CAS No.: 1443763-60-7

Empesertib (BAY-1161909, BAY1161909)

Catalog No.: PC-43261Not For Human Use, Lab Use Only.

Empesertib (BAY-1161909, BAY1161909) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.34 nM.

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Biological Activity

Empesertib (BAY-1161909, BAY1161909) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.34 nM.
BAY1161909 inhibits only JNK2 and JNK3 more than 50% at 1 uM in Millipore panel (230 kinases).
BAY1161909 abrogates nocodazole-induced metaphase arrest in HeLa cells with IC50 of 56 nM, inhibits the proliferation of a panel tumor cell lines covering various cancer with mean IC50 of 160 nM.
BAY1161909 enhances the efficacy of antimitotic cancer drugs and shows potentially overcome resistance in vivo.

Physicochemical Properties

M.Wt 559.6113
Formula C29H26FN5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 35 mg/mL

Chemical Name/SMILES

Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(methylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]pyridin-6-yl]phenyl]-α-methyl-, (αR)-

References

1. Wengner AM, et al. Mol Cancer Ther. 2016 Apr;15(4):583-92.

2. Uitdehaag JCM, et al. J Mol Biol. 2017 Jul 7;429(14):2211-2230.

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