885325-71-3

885325-71-3 structure

Name: MK-8745
Chemical Name: (3-Chloro-2-fluorophenyl)(4-{[6-(1,3-thiazol-2-ylamino)-2-pyridin yl]methyl}-1-piperazinyl)methanone
CAS Number: 885325-71-3
Molecular Formula: C₂₀H₁₉ClFN₅OS
Molecular Weight: 431.914
Catalog: Biochemical Inhibitor Cell Cycle Aurora Kinase Inhibitor
Create Date: 2017-05-14 12:58:55
Modify Date: 2024-01-05 10:22:04
MK-8745 is an aurora A kinase inhibitor with IC50s of 0.6 nM.

Name	(3-Chloro-2-fluorophenyl)(4-{[6-(1,3-thiazol-2-ylamino)-2-pyridin yl]methyl}-1-piperazinyl)methanone
Synonyms	(3-Chloro-2-fluorophenyl)(4-{[6-(1,3-thiazol-2-ylamino)-2-pyridinyl]methyl}-1-piperazinyl)methanone Methanone, (3-chloro-2-fluorophenyl)[4-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-piperazinyl]- MK-8745

Description	MK-8745 is an aurora A kinase inhibitor with IC50s of 0.6 nM.
Related Catalog	Research Areas >> Cancer
Target	Aurora A:0.6 nM (IC50)
In Vitro	MK-8745 induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages. Exposure of p53 wild-type cells to MK-8745 results in the induction of p53 phosphorylation (ser15) and an increase in p53 protein expression[1]. 1 μM of MK-8745 exposure for 24 h induces cell cycle arrest in all NHL cells, with variable degrees of G2/M arrest. Z138C cells are highly sensitive to MK-8745 (1 μ M) treatment and induces an approximate 5.5-fold increase in the G2/M phase cell population by 96 h. MK-8745 treatment inhibits phosphorylation of Aurora-A in Granta 519 and Z138C cells, while Akata and JVM2 has no effect. MK-8745 specifically inhibits Aurora-A specific function. MK-8745 treatment leads to apoptotic cell death[2].
Cell Assay	A total of 10000 cells are plated per well in a 96-well plate and treated with MK-8745 for varying time points starting 24 h after plating. Cell viability is measured by the MTT assay[2].
References	[1]. Jayasree S Nair et al. The induction of polyploidy or apoptosis by the Aurora A kinase inhibitor MK8745 is p53-dependent. [2]. Aparajita Chowdhury et al. A novel Aurora kinase A inhibitor MK-8745 predictsTPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines.Leuk Lymphoma, 2012 Mar, 53(3):462-71.