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细胞周期
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/ 驱动蛋白 / Ispinesib

伊斯平斯 /Ispinesib {[allProObj[0].p_purity_real_show]}

货号：A279561 同义名： 伊匹尼塞 / SB-715992;CK0238273

Ispinesib is a quinazolinone-derived, specific and reversible kinesin spindle protein inhibitor with Kiapp value of 1.7 nM.

Ispinesib 化学结构 CAS号：336113-53-2
Ispinesib 化学结构
CAS号：336113-53-2
Ispinesib 3D分子结构
CAS号：336113-53-2
Ispinesib 化学结构 CAS号：336113-53-2
Ispinesib 3D分子结构 CAS号：336113-53-2
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Ispinesib 纯度/质量文件 产品仅供科研

货号：A279561 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Kinesin ↓ 其他靶点 纯度
SB-743921 HCl ++++

KSP, Ki: 0.07 nM

KSP (P388 cells), IC50: 14.4 nM

 		99%+
GSK-923295 ++

CENP-E, Ki: 3.2 nM

 		99%+
Ispinesib +++

KSP (HsEg5), Ki app: 1.7 nM

 		99%+
AZ3146 +

Mps1, IC50: ~35 nM

 		98+%
MPI-0479605 ++

Mps1, IC50: 1.8 nM

 		99%+
BAY1217389 +++

Mps1, IC50: 0.63 nM

 		98%
ARQ 621 ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ispinesib 生物活性

靶点

  • Kinesin

    KSP (HsEg5), Ki app:1.7 nM
描述 Kinesins are motor proteins that have various of cellular physiologies, including mitosis, meiosis and cellular cargo transportation[1]. Ispinesib is a highly specific inhibitor of the kinesin spindle protein (KSP) with a median IC50 value of 5 nM[2].
The MDA-MB-468 cells (sensitive to ispinesib) and BT-474 cells(not sensitive to ispinesib) were treated with 150 nmol/L ispinesib and the expression of cell cycle markers (cyclin A, cyclin B and cyclin E) and apoptotic proteins (Bax, Bid, phospho-Bcl2, Bcl2 and Bcl-XL) were analyzed by western blotting at 0, 6, 16 and 48 hours. The expression of proteins Bax and Bid was higher in MDA-MB-468 cells and antiapoptitic protein Bcl-XL was lower. The marker of mitosis cyclin B was increased as the time increased in MDA-MB-468 cells but not in BT-474 cells. The cyclin E also increased after the ispinesib treatment on MDA-MB-468 cells[3].
CB17SC-M scid -/- female mice and BALB/c nu/nu mice with tumors xenografts were intraperitoneally administered Ispinesib (5 or 10 mg/kg) every 4 days for 3 doses repeated at day 21. Ispinesib could significantly delay the tumor growth in 88% and had intermediate 21% of solid tumor xenografts[4].
作用机制 The ability of KSP to bind to microtubules and the movement is changed and inhibited by ispinesib through preventing ADP release without inhibiting the release of the KSP-ADP complex from the microtubule[5].

Ispinesib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
human BxPC3 cells Growth inhibition assay 72 h Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay, GI50=0.08 μM 23394180
human BxPC3 cells Proliferation assay 72 h Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay, GI50=0.08 μM 22248262
human HCT116 cells Growth inhibition assay 72 h Growth inhibition of human HCT116 cells after 72 hrs by MTS assay, IC50=1.1 nM 26396688
human HeLa cells Proliferation assay 48 h Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=1 μM 24184776

Ispinesib 动物研究

Dose Mice: 10 mg/kg[3] (i.p.)
Administration i.p.

Ispinesib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00169520 Solid Tumor Cancer Phase 1 Completed - United Kingdom ... 展开 >> GSK Investigational Site Oxford, Oxfordshire, United Kingdom, OX2 6PD GSK Investigational Site London, United Kingdom, SW3 6JJ 收起 <<
NCT00607841 Breast Neoplasms Phase 1 Phase 2 Completed - Peru ... 展开 >> Hospital Nacional Alberto Sabogal Sologúren Lima, Peru Hospital Nacional Edgardo Rebagliati Martins Lima, Peru Instituto Nacional de Enfermedades Neoplásicas Lima, Peru 收起 <<
NCT00103311 - Completed - -

Ispinesib 参考文献

[1]Endow SA, Kull FJ, Liu H. Kinesins at a glance. J Cell Sci. 2010;123(Pt 20):3420-4.

[2]Sheth PR, Basso A, et al. Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein. Biochemistry. 2009;48(46):11045-55.

[3]Purcell JW, Davis J, et al. Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clin Cancer Res. 2010;16(2):566-76.

[4]Carol H, Lock R, et al. Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. Pediatr Blood Cancer. 2009;53(7):1255-63.

[5]Lad L, Luo L, et al. Mechanism of inhibition of human KSP by ispinesib. Biochemistry. 2008;47(11):3576-85.

Ispinesib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.67mL

1.93mL

0.97mL

19.34mL

3.87mL

1.93mL

Ispinesib 技术信息

CAS号336113-53-2
分子式C30H33ClN4O2
分子量 517.062
别名 伊匹尼塞 ;SB-715992;CK0238273
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 120 mg/mL(232.08 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Ispinesib | 336113-53-2 | SB-715992 | SB715992 | SB 715992 | KSP Inhibitor | Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis | Kinesin | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ispinesib 纯度/质量文件 | Ispinesib 亚型比较 | Ispinesib 生物活性 | Ispinesib 细胞研究 | Ispinesib 动物研究 | Ispinesib 临床数据 | Ispinesib 参考文献 | Ispinesib 实验方案 | Ispinesib 技术信息

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