1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. Zelavespib

Zelavespib  (Synonyms: PU-H71)

目录号: HY-11038 纯度: 99.90%
COA 产品使用指南

Zelavespib (PU-H71) 是一种有效的 Hsp90 抑制剂,在 MDA-MB-468 细胞中,对 Hsp90IC50 值为 51 nM。

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Zelavespib Chemical Structure

Zelavespib Chemical Structure

CAS No. : 873436-91-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥869
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5 mg ¥493
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10 mg ¥790
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50 mg ¥3600
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100 mg ¥7000
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500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.

IC50 & Target[1]

HSP90

51 nM (IC50, MDA-MB-468 cells)

体外研究
(In Vitro)

Zelavespib 是一种有效的 Hsp90 抑制剂,在 MDA-MB-468 细胞中的 IC50 为 51 nM。Zelavespib 抑制多种肿瘤细胞的生长,例如 MDA-MB-468、MDA-MB-231 和 HCC-1806 细胞,IC50s 为 65 ± 8 nM、140 ± 5 nM 和 分别为 87 ± 3 nM,这种抑制与 G2-M 阻滞相关。Zelavespib (10-1000 nM) 可诱导三阴性乳腺癌 (TNBC) 显着凋亡。Zelavespib (0.5, 1 μM) 还会下调参与 TNBC 侵袭潜力的癌蛋白[1]
Zelavespib (0.5 μM) 可减少并耗尽 BCR 信号激酶。Zelavespib (0.25-10 μM) 对 CLL 细胞具有细胞毒性,但对 PBMC 或静息 B 细胞影响极小。 此外,Zelavespib (0-1μM) 通过诱导线粒体凋亡来降低 CLL 活力,并在 0.5 μM 时拮抗来自 CLL 微环境的生存信号[2]
Zelavespib (0.05 μM) 诱导 MDA-MB-231、BT-474 和 MCF7 细胞凋亡,并且 TNF-α 可以增强这种诱导作用。 Zelavespib (0.05 μM) 可降解 IKKβ,并下调 TNF-α 处理诱导的 NF-κB 转录活性[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Zelavespib (75 mg/kg,腹膜内注射) 引起肿瘤内积聚,延长抗肿瘤驱动分子的下调,在 MDA-MB-468 荷瘤小鼠中以无毒剂量完成并保留反应。
Zelavespib(75 mg/kg,3×周,腹膜内注射)可抑制肿瘤的生长,这种作用与多种 Hsp90 调节的恶性驱动蛋白的下调有关[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

512.37

Formula

C18H21IN6O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (195.17 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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 1.9517 mL 9.7586 mL 19.5171 mL
5 mM 0.3903 mL 1.9517 mL 3.9034 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (4.88 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.88 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.90%

参考文献
Kinase Assay
[1]

Measurements are performed in black 96-well microtiter plates. In short, cell lysates are prepared by rupturing cellular membranes by freezing at -70°C and dissolving the cellular extract in HFB [20 mM Hepes (K), pH 7.3, 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 0.01% Nonidet P-40] with added protease and phosphatase inhibitors (Zelavespib, etc.). Saturation curves are recorded in which fluorescently labeled geldanamycin (Cy3B-GM) (3 nM) is treated with increasing amounts of cellular lysates. The amount of lysate that results in polarization (mP) readings corresponding to 90%-99% bound ligand is chosen for the competition study. Here, each 96-well plate contains 3 nM Cy3B-GM, cellular lysate and tested Hsp90 inhibitor in a final volume of 100 μL. The plate is left for 24 h on a shaker at 4°C, and the fluorescence polarization (FP) values in mP are recorded. EC50 values are determined as the competitor concentrations at which 50% of the Cy3B-GM is displaced. FP measurements are performed on an Analyst GT microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

The antiproliferative effects of select Hsp90 inhibitors is evaluated using the CellTiter-Glo Luminescent Cell Viability Assay kit. Briefly, exponentially growing MDA-MB-468, MDA-MB-231, and HCC-1806 cells are seeded into black 96-well microtiter plates and incubated in medium containing either vehicle control (DMSO) or Zelavespib for the indicated time at 37°C. Plates containing 3 replicate wells per assay condition are seeded at a density of 8 × 103 cells for each cell line in 100 μL medium. After exposure of cells to the Hsp90 inhibitors, plates are equilibrated to room temperature (20-25°C) for approximately 30 min, and 100 μL CellTiter-Glo reagent are added to each well. Plates are mixed for 2 min on an orbital shaker and then incubated for 15 min to 2 h at room temperature. The luminescence signal in each well is measured in an Analyst GT microplate reader. The percentage cell growth inhibition is calculated by comparing luminescence readings obtained from treated versus control cells, accounting for initial cell population (time 0). The IC50 is calculated as the drug concentration that inhibits cell growth by 50%[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Mice bearing MDA-MB-468 tumors reaching a volume of 100-150 mm3 are treated i.p. using different doses and schedules: Group 01 (n = 8) PBS; group 02 (n = 8) Zelavespib at 50 mg/kg on alternate days; group 03 (n = 8) Zelavespib at 50 mg/kg 5xqd; group 04 (n = 8) Zelavespib at 75 mg/kg 3 week; group 05 (n = 8) Zelavespib at 75 mg/kg on alternate days. Mice bearing HCC-1806 or MDA-MB-231 xenografted tumors receive Zelavespib at 75 mg/kg on alternate days. Tumor volume is determined by measurement with Vernier calipers, and tumor volume is calculated as the product of its length × width2 × 0.4. Tumor volume is expressed on indicated days as the median tumor volume ± SD indicated for groups of mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9517 mL 9.7586 mL 19.5171 mL 48.7929 mL
5 mM 0.3903 mL 1.9517 mL 3.9034 mL 9.7586 mL
10 mM 0.1952 mL 0.9759 mL 1.9517 mL 4.8793 mL
15 mM 0.1301 mL 0.6506 mL 1.3011 mL 3.2529 mL
20 mM 0.0976 mL 0.4879 mL 0.9759 mL 2.4396 mL
25 mM 0.0781 mL 0.3903 mL 0.7807 mL 1.9517 mL
30 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6264 mL
40 mM 0.0488 mL 0.2440 mL 0.4879 mL 1.2198 mL
50 mM 0.0390 mL 0.1952 mL 0.3903 mL 0.9759 mL
60 mM 0.0325 mL 0.1626 mL 0.3253 mL 0.8132 mL
80 mM 0.0244 mL 0.1220 mL 0.2440 mL 0.6099 mL
100 mM 0.0195 mL 0.0976 mL 0.1952 mL 0.4879 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-11038
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