2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Icapamespib

Icapamespib  (Synonyms: PU-HZ151)

目录号: HY-137441 纯度: 99.52%
COA 产品使用指南 技术支持

Icapamespib (PU-HZ151; PU-AD) 是一种选择性、口服有效、靶向 HSP90 组装的病理伴侣复合物 (Epichaperomes) 抑制剂，具有慢解离动力学特性。Icapamespib 可通过血脑屏障 (BBB)，通过非共价结合 HSP90，诱导epichaperomes 解体，恢复正常蛋白-蛋白相互作用网络。Icapamespib 可特异性破坏疾病相关的异常蛋白互作网络，减少神经毒性蛋白聚集和肿瘤细胞存活信号。Icapamespib 可用于阿尔茨海默病等神经退行性疾病及胶质母细胞瘤、转移性乳腺癌等研究。

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Icapamespib Chemical Structure

Icapamespib Chemical Structure

CAS No. : 1000999-96-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4050
In-stock
1 mg ￥1400
In-stock
5 mg ￥3500
In-stock
10 mg ￥5500
In-stock
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100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Icapamespib:

Icapamespib 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Icapamespib (PU-HZ151; PU-AD) is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib can cross the blood-brain barrier (BBB) ??and induce epichaperome disassembly by non-covalently binding to HSP90, restoring the normal protein-protein interaction network. Icapamespib can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib can be used in the research of neurodegenerative diseases such as Alzheimer's disease, as well as cancers such as glioblastoma and metastatic breast cancer[1][2][3].

IC50 & Target

HSP90

 

体外研究
(In Vitro)

Icapamespib 在 MDA-MB-468 细胞匀浆中对 Epichaperomes 的 EC50 为 5 nM，结合亲和力高于 PU-H71 (EC50 为 11 nM)[1]。
Icapamespib (0.1-1 μM；24 h) 可显著降低 MDA-MB-468 细胞活力，并通过破坏 Epichaperome 结构减少高分子量 HSP90 复合物，同时诱导 p-ERK 磷酸化水平下降及 c-PARP 剪切[1]。

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

Icapamespib 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-468, ASPC1
Concentration: 1 μM
Incubation Time: 1 h
Result: Reduced the formation of high-molecular-weight HSP90 complexes in native-PAGE analysis, while total HSP90 levels remain unchanged in SDS-PAGE, indicating specific disruption of epichaperomes without altering total chaperone expression.
体内研究
(In Vivo)

Icapamespib (10 mg/kg；静脉注射；每周 2 次；3 周) 显著抑制人胶质母细胞瘤 U87MG 荷瘤裸鼠模型的肿瘤生长，缩肿瘤体积小，且未观察到明显毒性[1]。
Icapamespib 可靶向阿尔兹海默症和脚趾母细胞瘤[2]。
124I 标记的 PU-AD (Icapamespib) 衍生物已用于通过 PET 成像检测和量化体内表分子伴侣 (Epichaperomes)[2]。

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

Animal Model: Female BALB/c nude mice (6-8 weeks old, 18-20 g) bearing U87MG glioblastoma xenografts[1]
Dosage: 10 mg/kg
Administration: Intravenous injection via tail vein, twice weekly for 3 weeks.
Result: Significantly reduced tumor volume by 65% compared to vehicle controls.
Decreased levels of HSP90 client proteins (EGFR, AKT) and increased HSP70 expression.
No significant body weight loss or organ toxicity was observed.
Clinical Trial
分子量

526.39

Formula

C19H23IN6O2S
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (189.97 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 1.8997 mL 9.4987 mL 18.9973 mL
5 mM 0.3799 mL 1.8997 mL 3.7995 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

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

只
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
纯度 & 产品资料

纯度: 99.52%

COA (293 KB) HNMR (264 KB) LCMS (268 KB)

产品使用指南 (1538 KB)
参考文献

Icapamespib 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。-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 1.8997 mL 9.4987 mL 18.9973 mL 47.4933 mL
5 mM 0.3799 mL 1.8997 mL 3.7995 mL 9.4987 mL
10 mM 0.1900 mL 0.9499 mL 1.8997 mL 4.7493 mL
15 mM 0.1266 mL 0.6332 mL 1.2665 mL 3.1662 mL
20 mM 0.0950 mL 0.4749 mL 0.9499 mL 2.3747 mL
25 mM 0.0760 mL 0.3799 mL 0.7599 mL 1.8997 mL
30 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5831 mL
40 mM 0.0475 mL 0.2375 mL 0.4749 mL 1.1873 mL
50 mM 0.0380 mL 0.1900 mL 0.3799 mL 0.9499 mL
60 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7916 mL
80 mM 0.0237 mL 0.1187 mL 0.2375 mL 0.5937 mL
100 mM 0.0190 mL 0.0950 mL 0.1900 mL 0.4749 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.

Keywords:

Icapamespib1000999-96-1PU-HZ151HSPHeat shock proteinsInhibitorinhibitorinhibit

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