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/ 驱动蛋白 / Ispinesib/伊斯平斯

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

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

Ispinesib是一种源自喹唑啉酮的特异性且可逆的有丝分裂纺锤蛋白抑制剂，Ki值为1.7 nM。

Ispinesib/伊斯平斯 化学结构 CAS号：336113-53-2
Ispinesib/伊斯平斯 化学结构
CAS号：336113-53-2
Ispinesib/伊斯平斯 3D分子结构
CAS号：336113-53-2
Ispinesib/伊斯平斯 化学结构 CAS号：336113-53-2
Ispinesib/伊斯平斯 3D分子结构 CAS号：336113-53-2
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Ispinesib/伊斯平斯 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 (P388 cells), IC50: 14.4 nM

KSP, Ki: 0.07 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/伊斯平斯 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/伊斯平斯 细胞实验

Cell Line
Concentration Treated Time Description References
K562 cells 100 nM To assess the inhibitory effects on cancer cell lines. J Med Chem. 2012 Feb 23;55(4):1511-25.
HeLa cells 10 nM to 100 nM 10 days To validate the A133P mutation's resistance to Ispinesib via CRISPR/Cas9 genome editing Nat Chem Biol. 2014 Aug;10(8):626-8.
HCT116 cells 50 – 125 nM 2 to 4 weeks To select resistant clones and analyze their resistance mechanisms Nat Chem Biol. 2014 Aug;10(8):626-8.
MDA-MB-468 cells 150 mM 48 hours To evaluate the cell cycle and apoptotic responses of MDA-MB-468 cells to Ispinesib, results showed cell cycle arrest at M phase and induction of apoptosis. Clin Cancer Res. 2010 Jan 15;16(2):566-76.
BT-474 cells 150 mM 48 hours To evaluate the cell cycle and apoptotic responses of BT-474 cells to Ispinesib, results showed transient cell cycle arrest at M phase followed by re-entry into interphase. Clin Cancer Res. 2010 Jan 15;16(2):566-76.
HeLa cells 1 nM 72 hours To evaluate the inhibitory effect of Ispinesib on HeLa cell proliferation, results showed that Ispinesib synergistically inhibited cell proliferation with KIF15-IN-1. Proc Natl Acad Sci U S A. 2018 May 15;115(20):E4613-E4622.

Ispinesib/伊斯平斯 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Breast cancer xenograft models Intraperitoneal injection 10 mg/kg or 8 mg/kg Every 4 days for 3 doses To evaluate the antitumor activity of Ispinesib in breast cancer xenograft models, results showed tumor regression in all models, with complete regression in some models. Clin Cancer Res. 2010 Jan 15;16(2):566-76.

Ispinesib/伊斯平斯 动物研究

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

Ispinesib/伊斯平斯 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/伊斯平斯 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/伊斯平斯 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/伊斯平斯 技术信息

CAS号336113-53-2
分子式C30H33ClN4O2
分子量 517.06
SMILES Code O=C(N(CCCN)[C@@H](C(N1CC2=CC=CC=C2)=NC3=C(C=CC(Cl)=C3)C1=O)C(C)C)C4=CC=C(C)C=C4
MDL No. MFCD22628831
别名 伊匹尼塞 ;SB-715992; CK0238273
运输蓝冰
InChI Key QJZRFPJCWMNVAV-HHHXNRCGSA-N
Pubchem ID 6851740
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

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/伊斯平斯 纯度/质量文件 | Ispinesib/伊斯平斯 亚型比较 | Ispinesib/伊斯平斯 生物活性 | Ispinesib/伊斯平斯 动物研究 | Ispinesib/伊斯平斯 临床数据 | Ispinesib/伊斯平斯 参考文献 | Ispinesib/伊斯平斯 实验方案 | Ispinesib/伊斯平斯 技术信息

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