AZ3146 是一种有效的 Mps1 和 TTK 抑制剂，IC₅₀ 为 35 nM (Mps1^Cat)。

AZ3146 is a reasonably potent Mps1 and TTK inhibitor, with IC 50 of 35 nM for Mps1.

Solid

Mps1 35 nM (IC50)

In in vitro kinase assays, AZ3146 inhibits human Mps1 with IC50 of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells. 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. 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-fo

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.
[2]. Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.

In Vitro: DMSO : 100 mg/mL (220.97 mM; Need ultrasonic)配制储备液