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

Icapamespib hydrochloride  (Synonyms: PU-HZ151 hydrochloride)

目录号: HY-137441A 纯度: 98.67%
COA 产品使用指南 技术支持

Icapamespib (PU-HZ151; PU-AD) hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride Chemical Structure

Icapamespib hydrochloride Chemical Structure

CAS No. : 2267287-26-1

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1 mg ￥1400
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5 mg ￥3500
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10 mg ￥5500
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Customer Review

Other Forms of Icapamespib hydrochloride:

Icapamespib hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

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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) hydrochloride is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib hydrochloride 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 hydrochloride can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib hydrochloride 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 hydrochloride 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 hydrochloride (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 hydrochloride 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) hydrochloride 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 hydrochloride 可靶向阿尔兹海默症和脚趾母细胞瘤[2]。
124I 标记的 Icapamespib hydrochloride 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 Icapamespib
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.
分子量

599.32

同用名

PU-HZ151 hydrochloride

Formula

C19H25Cl2IN6O2S
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

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 : 9.09 mg/mL (15.17 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6686 mL 8.3428 mL 16.6856 mL
5 mM 0.3337 mL 1.6686 mL 3.3371 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
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
参考文献

Icapamespib 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 1.6686 mL 8.3428 mL 16.6856 mL 41.7139 mL
5 mM 0.3337 mL 1.6686 mL 3.3371 mL 8.3428 mL
10 mM 0.1669 mL 0.8343 mL 1.6686 mL 4.1714 mL
15 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7809 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.

Keywords:

Icapamespib2267287-26-1PU-HZ151HSPHeat shock proteinsHSP90Inhibitorinhibitorinhibit

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