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| 品牌 | absin | CAS | 1124329-14-1 |
|---|---|---|---|
| 分子式 | C24H32N6O3 | 纯度 | ＞98% |
| 分子量 | 452.55 | 货号 | abs810391 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a potent and selective monopolar spi | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AZ3146 1124329-14-1
| 产品描述 | |
| 描述 | AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM); less potent to FAK, JNK1, JNK2, and Kit. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | AZ 3146；AZ-3146 |
| 外观 | white to light brown powder |
| 可溶性/溶解性 | DMSO : 11.3 mg/mL (25 mM) Ethanol : 33.9 mg/mL (75 mM) |
| 生物活性 | |
| 靶点 | Mps1 |
| In vitro(体外研究) | 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. 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-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. |
| 研究领域 | |
| 研究领域 | CancerDrug resistance CancerTumor biomarkers Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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