Ispinesib (Synonyms:伊斯平斯; SB-715992)
目录号 : KM16370 CAS No. : 336113-53-2 纯度 : 98%

Ispinesib 是一种特异性的纺锤体驱动蛋白 KSP 抑制剂,Ki app 值为 1.7 nM。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.

体外研究

Ispinesib is a potent, highly specific inhibitor of KSP, with a Ki app of 1.7 nM. Ispinesib (150 nM) inhibits BT-474 and MDA-MB-468 cell lines, with GI50s of 45 and 19 nM, respectively. Ispinesib (SB715992, 15 and 30 nM) suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib can be enhanced by genistein.

体内研究

Ispinesib (SCID, 8 mg/kg; nude, 10 mg/kg, q4d × 3) reduces tumor volume in mice bearing tumor xenografts of ER-positive (MCF7), HER2-positive (KPL4, HCC1954, and BT-474), and triple-negative (MDA-MB-468) breast cancer cells via i.p. one dose every 4 days repeated three times.

分子式
C30H33N4O2Cl
分子量
517.06
CAS号
336113-53-2
中文名称
伊斯平斯;伊匹尼塞
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : ≥ 125 mg/mL (241.75 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9340 mL 9.6701 mL 19.3401 mL
5 mM 0.3868 mL 1.9340 mL 3.8680 mL
10 mM 0.1934 mL 0.9670 mL 1.9340 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.84 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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