CAS NO: | 1124329-14-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | AZ3146 is a reasonably potentMps1and TTK inhibitor, withIC50of 35 nM forMps1Cat. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | In in vitro kinase assays, AZ3146 inhibits human Mps1Catwith IC50of ~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 GI50of approximately 3 μM (4-fold resistance), while the remaining clones have a GI50of 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]. | ||||||||||||||||
分子量 | 452.55 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H32N6O3 | ||||||||||||||||
CAS 号 | 1124329-14-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(220.97 mM;Need ultrasonic) 配制储备液
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