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HMN176 是一种二苯乙烯衍生物,可抑制有丝分裂,干扰 polo 样激酶-1 (PLK1)
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HMN176 是一种二苯乙烯衍生物,可抑制有丝分裂,干扰 polo 样激酶-1 (PLK1)
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 313 | 现货 | |
2 mg | ¥ 463 | 现货 | |
5 mg | ¥ 828 | 现货 | |
10 mg | ¥ 1,230 | 现货 | |
25 mg | ¥ 1,980 | 现货 | |
50 mg | ¥ 3,710 | 现货 | |
100 mg | ¥ 5,330 | 现货 | |
500 mg | ¥ 10,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 718 | 现货 |
产品描述 | HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1). |
体外活性 | HMN-176(2.5μM)显著延长了hTERT-RPE1和CFPAC-1细胞系的有丝分裂持续时间。HMN-176对纺锤体形态的影响似乎与微管聚合作用无关。通过浓度依赖方式,HMN-176(2.5,0.25,和0.025μM)抑制星状体的形成[1]。HMN-176(0.1,1.0,或10.0 µg/mL)在多种肿瘤样本中显示出抑制效果,特别是在乳腺癌、非小细胞肺癌和卵巢癌样本中表现出显著活性。在10.0 µg/mL的处理浓度下,HMN-176对63%的乳腺癌(5/8)、67%的非小细胞肺癌(4/6)和57%的卵巢癌(4/7)肿瘤样本表现出活性[2]。HMN-176展示出强大的细胞毒性,平均IC50值为118 nM,并且对来自不同器官具有不同特性的肿瘤显示出类似的细胞毒性[3]。3μM HMN-176处理抑制MDR1 mRNA表达56%,对剩余的启动子活性无显著影响[4]。 |
体内活性 | HMN-176通过抑制以中心体为依赖的MT(微管蛋白)核形成,即星体形成,防止Spisula卵母细胞的纺锤体组装和减数分裂。用0.25 μM HMN-176处理的卵母细胞会发生GVBD,但即使经过长时间,星体或纺锤体也无法形成[1]。雄性大鼠口服HMN-214后,在血浆中检测不到该前药,而HMN-176在血浆中的浓度在2小时达到峰值,之后逐渐降低[3]。 |
细胞实验 | Cells to be tested are seeded into a 96-well microplate at a density of 3 ×103-1×104 cells/well. Drugs are added the next day and the plate is incubated for 72 h at 37 °C in a humidified incubator (5% CO2, 95% air). The inhibition of growth is measuredby the MTT assay, and the concentration required to produce 50% inhibition of growth (IC50) calculated by the Scansoft 96 software program. The IC50 values for HMN-176 andreference agents are presented. Briefly, for each compound the mean IC50 value for all cell lines tested is calculated and the difference between the individual IC50 values and the mean IC50 value (log10) displayed by a bar projecting to the right or left of the mean. The resistance index is calculated as (IC50 value for drug-resistant cell line)/(IC50 for parent cell line). |
分子量 | 382.43 |
分子式 | C20H18N2O4S |
CAS No. | 173529-10-7 |
Smiles | COc1ccc(cc1)S(=O)(=O)Nc1ccccc1\C=C\c1cc[n+]([O-])cc1 |
密度 | 1.24 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (130.74 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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