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

Zelavespib hydrochloride  (Synonyms: PU-H71 hydrochloride)

目录号: HY-11038B 纯度: 98.89%
COA 产品使用指南

Zelavespib (PU-H71) hydrochloride 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 hydrochloride Chemical Structure

Zelavespib hydrochloride Chemical Structure

CAS No. : 2095432-24-7

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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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Customer Review

Other Forms of Zelavespib hydrochloride:

  • 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) hydrochloride 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 hydrochloride 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

548.83

Formula

C18H22ClIN6O2S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 15.38 mg/mL (28.02 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8221 mL 9.1103 mL 18.2206 mL
5 mM 0.3644 mL 1.8221 mL 3.6441 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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

动物实验:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 14.29 mg/mL (26.04 mM); 澄清溶液; 超声助溶

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
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.89%

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

Zelavespib hydrochloride 相关分类

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 (sealed storage, away from moisture)。-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
H2O 1 mM 1.8221 mL 9.1103 mL 18.2206 mL 45.5514 mL
5 mM 0.3644 mL 1.8221 mL 3.6441 mL 9.1103 mL
10 mM 0.1822 mL 0.9110 mL 1.8221 mL 4.5551 mL
15 mM 0.1215 mL 0.6074 mL 1.2147 mL 3.0368 mL
20 mM 0.0911 mL 0.4555 mL 0.9110 mL 2.2776 mL
25 mM 0.0729 mL 0.3644 mL 0.7288 mL 1.8221 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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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