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TAI1 是一种具有口服活性的特异性 Hec1 抑制剂,有抗肿瘤活性,在 K562 细胞中的 GI50值为 13.48 nM。
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TAI1 是一种具有口服活性的特异性 Hec1 抑制剂,有抗肿瘤活性,在 K562 细胞中的 GI50值为 13.48 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 295 | 现货 | |
5 mg | ¥ 747 | 现货 | |
10 mg | ¥ 1,230 | 现货 | |
25 mg | ¥ 2,490 | 现货 | |
50 mg | ¥ 3,490 | 现货 | |
100 mg | ¥ 5,120 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction. |
靶点活性 | K562 cells:13.48 nM (GI50) |
体外活性 | TAI-1通过干扰Nek2与Hec1的结合,引起Nek2的降解和染色体错位。TAI-1在多种肿瘤细胞中以nM水平显示出强大的生长抑制效力,并且在白血病、乳腺癌和肝癌细胞中与多柔比星、拓扑替康和紫杉醇产生协同作用。[1] |
体内活性 | TAI-1(20 mg/kg 静脉注射或150 mg/kg 口服)在Huh-7模型中显著延缓肿瘤生长,在Colo205和MDA-MB-231模型中轻微抑制肿瘤增长。[1] |
细胞实验 | Cells are seeded in 96 well plates, incubated for 24 hours, compounds added and incubated for 96 hours. All testing points are tested in triplicate wells. Cell viability is determined by MTS assay using CellTiter 96? Aqueous Non-radioactive Cell Proliferation Assay system according to manufacturer's instructions with MTS and PMS. Data retrieved from spectrophotometer are processed in Excel and GraphPad Prism 5 to calculate the concentration exhibiting 50% growth inhibition (GI50). All data represent the results of triplicate experiments.(Only for Reference) |
分子量 | 431.51 |
分子式 | C24H21N3O3S |
CAS No. | 1334921-03-7 |
Smiles | COc1ccc(Oc2cc(C)c(-c3csc(NC(=O)c4ccncc4)n3)c(C)c2)cc1 |
密度 | 1.281 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: 80 mg/mL (185.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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