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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
K858
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
72926-24-0
- 规格：
50mg/25mg/10mg/5mg
| 规格： | 50mg | 产品价格： | ￥2590.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥1590.0 |
| 规格： | 10mg | 产品价格： | ￥790.0 |
| 规格： | 5mg | 产品价格： | ￥490.0 |
是一种 ATP 非竞争性的驱动蛋白 Eg5 抑制剂。
| 基本信息 | |
| CAS | No.72926-24-0 |
| 中文名称 | N-(4-乙酰基-4,5-二氢-5-甲基-5-苯基-1,3,4-噻二唑-2-基)乙酰胺 |
| 英文名称 | K858 |
| 分子式 | C13H15N3O2S |
| 分子量 | 277.34 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 货期 | 1-2个工作日 |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00181155 |
| SMILES | CC(NC1=NN(C(C)=O)C(C2=CC=CC=C2)(C)S1)=O |
| InChIKey | JEFVYQYZCAVNTP-UHFFFAOYSA-N |
| InChI | InChI=1S/C13H15N3O2S/c1-9(17)14-12-15-16(10(2)18)13(3,19-12)11-7-5-4-6-8-11/h4-8H,1-3H3,(H,14,15,17) |
| PubChem CID | 2930014 |
| 靶点 | Kinesin;Eg5 |
| 通路 | Cytoskeleton |
| 背景说明 | K858是一种 ATP 非竞争性的驱动蛋白 Eg5 抑制剂。 |
| 生物活性 | K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.[1-2] |
| 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[1]. 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[2]. |
| 细胞实验 | 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[1]. |
| 细胞实验 | To determine cytotoxicity， sulforhodamine B colorimetric assay is performed: 1.5 × 104 cells are plated on 96 well plates， grown for 24 h (h) and treated with different concentrations of K858 (1 μM， 10 μM， 100 μM) for 24 and 48 h. Cells are then fixed with 50 % trichloroacetic acid for 1 h at 4°C and stained for 30 min at room temperature (RT) with 0.4 % sulforhodamine B in 1 % acetic acid. Excess dye is removed by washing four times with 1 % acetic acid. Protein bound dye is dissolved in 10 mM TRIS pH 10， and optical density (OD) is determined at 510 nm using a microplate reader[2]. |
| 动物实验 | A2780 cells (5 × 106 cells) are inoculated s.c. into BALB/cAJcl-nu mice. K858 is administered orally twice daily on days 0 to 4， and 7 to 11 at 150 and 50 mg/kg. Doses and schedules are determined by the tolerability studies performed in advance. Vehicle (0.5% methylcellulose 400) is administered orally as a control twice daily on days 0 to 4， and 7 to 11. Paclitaxel is administered i.v. on day 0 at 25 mg/kg. Carboplatin is administered i.v. on day 0 at 60 mg/kg. Drug efficacy is expressed as the ratio of the mean experimental V/V0 value to that of the control group [treated versus control (T/C) ratio]， where V is the tumor volume at the day of evaluation and V0 is the tumor volume at the day of the initial treatment with the drug. Statistical analysis is performed using the nonparametric rank-sum test[1]. |
| 数据来源文献 | [1]. Nakai R， et al. K858， a novel inhibitor of mitotic kinesin Eg5 and antitumor agent， induces cell death in cancer cells. Cancer Res. 2009 May 1;69(9):3901-9. [2]. De Iuliis F， et al. The kinesin Eg5 inhibitor K858 induces apoptosis but also survivin-related chemoresistance in breast cancer cells. Invest New Drugs. 2016 Aug;34(4):399-406. |
| 单位 | 瓶 |
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它是何种氨基酸。Sanger用此方法测定了胰岛素的N�末端分别为甘氨酸及苯丙氨酸。 B.氰酸盐法：1963年Stank及Smyth介绍了一种测定N�末端的新方法，步骤如下： 由于乙内酰脲氨基酸不带电荷，因此可用离子交换层析法将它与游离氨基酸分开，分离所得的乙内酰脲氨基酸再被盐酸水解，重新生成游离的氨基酸，鉴别此氨基酸即可了解N-末端是何种氨基酸。 C.二甲基氨基萘磺酰氯法：1956年Hartley等报告了一种测定N-末端的灵敏方法，采用1-二甲基氨基萘-5
）：ADP或某些其它的核苷-5′—二磷酸的磷酸化是通过来自一个非核苷酸底物的磷酰基的转移实现的。这种磷酸化与电子的转递链无关。 5，柠檬酸循环（citric acid cycle）：也称为三羧酸循环（TAC），Krebs循环。是用于乙酰CoA中的乙酰基氧化成CO2的酶促反应的循环系统，该循环的第一步是由乙酰CoA经草酰乙酸缩合形成柠檬酸。 6，回补反应(anaplerotic reaction)：酶催化的，补充柠檬酸循环中间代谢物供给的反应，例如由丙酮酸羧化酶生成草酰乙酸的反应。 7，乙醛酸循环
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