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1124329-14-1 | AZ3146

AZ3146 NLT 98%

SKU : MC507121

CAS Number : 1124329-14-1

Molecular Formula : C24H32N6O3 | Molecular Weight : 452.55

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name AZ3146
CAS Number 1124329-14-1
MDL Number MFCD18384959
Molecular Formula C24H32N6O3
Molecular Weight 452.55
Introduction of 1124329-14-1 :

AZ3146 is a reasonably potent and selective Mps1 inhibitor with IC50 of 35 nM for Mps1Cat. IC50 & Target: IC50: 35 nM (Mps1)[1] In Vitro: In in vitro kinase assays, AZ3146 inhibits human Mps1Cat with IC50 of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells[1]. TTK specific kinase inhibitor AZ3146 can decrease HCC cell growth. In vitro cell cytotoxicity assays are performed on SMMC-7721 and BEL-7404 cells. IC50s are calculated as being 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). Both cells are further treated under the concentration of IC50 for 4 days. Significant inhibitions of cell proliferation are observed[2]. HCT116 cells are cultured for 10 days in 0.8 μM (the GI50) of AZ3146 , then 2 μM AZ3146 for 3 weeks. Sixteen clones are isolated and cell lines generated, named AzR1-16, all of which are resistant to AZ3146-induced cell death in cell viability assays; AzR3 and 4 have a GI50 of approximately 3 μM (4-fold resistance), while the remaining clones have a GI50 of approximately 9 μM (11-fold resistance). When analyzing mitosis by time-lapse microscopy, while 2 μM AZ3146 causes the parental cell line to rapidly exited mitosis in 10 minutes[3].

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