伊斯平斯|T2103|TargetMol

Ispinesib
336113-53-2

￥247 1mg 起订

￥695 5mg 起订

￥1160 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 伊斯平斯

英文名称：: Ispinesib

CAS号：: 336113-53-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.57%

产品类别：: 抑制剂

货号：: T2103

Product Introduction

Bioactivity

名称	Ispinesib
描述	Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.
细胞实验	Cells are plated in log phase of growth in 96-well plates and treated with Ispinesib for 72 hours. Then, cell growth is measured using CellTiter-Glo, and luminescence is detected using BioTek FLx800. Data are analyzed and the IC50 value, defined as the drug concentration that results in 50% growth inhibition relative to control, is calculated.(Only for Reference)
激酶实验	Steady-State Kinetic Analysis of Human KSP ATPase Activity and Inhibition by Ispinesib: Kinesin specificity analysis is carried out using a pyruvate kinase-lactate dehydrogenase detection system that couples the production of ADP to oxidation of NADH. Absorbance changes are monitored at 340 nm. Steady-state studies using nanomolar concentrations of KSP are performed using a sensitive fluorescence-based assay utilizing a pyruvate kinase, pyruvate oxidase, and horseradish peroxidase (HRP) coupled detection system that couples the generation of ADP to oxidation of Amplex Red to fluorescent resorufin. Generation of resorufin is monitored by fluorescence (λexcitation = 520 nm and λemission = 580 nm). Steady-state biochemical experiments are performed in PEM25 buffer [25 mM Pipes-K+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel for experiments involving microtubules. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM Microtubules, and 1 nM KSP in PEM25 buffer. Ki app (apparent inhibitor dissociation constant) values of Ispinesib are extracted from the dose-response curves, with explicit correction for enzyme concentration by using the Morrison equation. Inhibitor modality (e.g., competitive, noncompetitive, uncompetitive, or mixed) under steady-state conditions is determined by measuring the effect of inhibitor concentration on initial velocity as a function of substrate concentrations. Data are fit using equations in GraFit to velocity equations for the various modes of inhibition.
体外活性	携带移植瘤的小鼠模型, Ispinesib（4.5-15 mg/kg）能够抑制Colo205, Colo201, HT-29细胞生长.在小鼠实体瘤中,用Ispinesib处理（6 -10 mg/kg ）,Madison 109肺癌, M5076肉瘤,及L1210和P388白血病能够被抑制.携带乳腺癌细胞MCF-7, HCC1954, MDA-MB-468,和KPL4移植瘤的小鼠中,Ispinesib（8-10 mg/kg ）抑制肿瘤生长.
体内活性	在PC-3前列腺癌细胞中, Ispinesib（5 nM 和 30 nM）通过调节信号的基因表达水平,抑制细胞增殖和诱导细胞凋亡。在乳腺癌细胞系中, Ispinesib（7.4 nM–600 nM）具有广谱抑制活性。在肿瘤细胞系中（Colo205, Colo201, HT-29, M5076, Madison-109,和MX-1）,Ispinesib（IC50=1.2-9.5 nM）具有很强细胞毒性。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 95 mg/mL (183.7 mM) DMSO : 95 mg/mL (183.7 mM)
关键字	CK-0238273 \| inhibit \| SB715992 \| Ispinesib \| Kinesin \| Inhibitor \| CK 0238273 \| SB 715992 \| Apoptosis
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伊斯平斯|||伊匹尼塞|||SB-715992|||CK0238273|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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