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AZ3146

目录号: PL07535 纯度: ≥99%

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

CAS No. :1124329-14-1

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中文名称	AZ3146
中文别名	9-环戊基-2-[[2-甲氧基-4-[(1-甲基哌啶-4-基)氧基]-苯基]氨基]-7-甲基-7,9-二氢-8H-嘌呤-8-酮;9-环戊基-7,9-二氢-2-[[2-甲氧基-4-[(1-甲基-4-哌啶基)氧基]苯基]氨基]-7-甲基-8H-嘌呤-8-酮;AZ3146 抑制剂
英文名称	AZ3146
英文别名	8H-Purin-8-one, 9-cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]amino]-7-methyl-;AZ 3146;AZ-3146;8H-Purin-8-one, 9-cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]...;AZ 3146 (AZ-3146);hesperadine;9-cyclopentyl-2-({2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl}amino)-7-methyl-7,9-dihydro-8H-purin-8-one;9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one;CS-0883;9-Cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]amino]-7-methyl-8H-purin-8-one;AZ3146;9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one;AK174927;9-cyclopentyl-2-[2-methoxy-4-(1-methylpiperidin-4-yl)oxyanilino]-7-methylpurin-8-one;9-cyclopentyl-2-({2-methoxy-4-[(1-methyl
Cas No.	1124329-14-1
分子式	C₂₄H₃₂N₆O₃
分子量	452.55
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	AZ3146 是一种有效的 Mps1 和 TTK 抑制剂，IC50 为 35 nM (Mps1^Cat)。

产品详情	AZ3146 是一种有效的 Mps1 和 TTK 抑制剂，IC₅₀ 为 35 nM (Mps1^Cat)。
生物活性	AZ3146 is a reasonably potent Mps1 and TTK inhibitor, with IC 50 of 35 nM for Mps1.
性状	Solid
IC50 & Target[1][2]	Mps1 35 nM (IC50)
体外研究(In Vitro)	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
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

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

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AZ3146

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