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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
72926-24-0
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥550.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥500.0 |
| 规格： | 10 mg | 产品价格： | ￥900.0 |
| 规格： | 25 mg | 产品价格： | ￥1950.0 |
| 规格： | 50 mg | 产品价格： | ￥3500.0 |
| 规格： | 100 mg | 产品价格： | ￥6400.0 |
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K858 (Racemic)
CAS No. : 72926-24-0
MCE 国际站：K858 (Racemic)
产品活性：K858 Racemic 是一种 ATP 非竞争性的驱动蛋白 Eg5 抑制剂，IC50 值为 1.3 μM。
研究领域：Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis
In Vitro: K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM. K858 does not inhibit the ATPase activity of the mitotic kinesins CENP-E and MKLP1, or the conventional kinesin heavy chain even at 200 μM. K858 induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines. Furthermore, the up-regulation of survivin is totally reversed by wortmannin (phosphoinositide 3-kinase AKT) in MCF7 cells.
In Vivo: K858 (50, 150 mg/kg, p.o.) shows antitumor activity in an A2780 ovarian cancer xenograft model, also inhibits tumor grwoth in a HCT116 colon cancer xenograft model via 100 mg/kg twice a day orally for 5 days. K858 (100 mg/kg, p.o., qd ×5) displays no neurotoxic side effects in mice.
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文献和实验消旋体 racemic modification 由等量对映体构成的光学不活性的物体。结晶时有右旋微结晶和左旋微结晶的单纯混合物的状态，以及在结晶的单位格子中对映体分子各以相同数目存在的情况。
Resolving Racemic Mixtures Using Parallel Combinatorial Libraries
As human enzymes and cell surface receptors possess handedness, the enantiomers of a racemic pair of compounds may be absorbed, activated, and degraded in different manners. In some instances, two enantiomers of a racemic drug
on the relative ease of method development and high likelihood of success for obtaining acceptable chromatographic performance while providing short analysis time. In this chapter, we describe the separation of racemic 1-(9-Anthryl)-2,2,2-trifluoroethanol
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