Icapamespib hydrochloride
Based on 1 publication(s) in Google Scholar
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.
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- Pureté : 98.74%
- CAS No.: 2267287-26-1
- Formule: C19H25Cl2IN6O2S
- Masse moléculaire:599.32
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Icapamespib hydrochloride
More
Activité biologique
Description
IC50 & Target
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HSP90 |
In Vitro
Icapamespib hydrochloride has an EC50 of 5 nM for epichaperomes in MDA-MB-468 cell homogenates, with a higher binding affinity than PU-H71 (EC50 of 11 nM)[1].
Icapamespib hydrochloride (0.1-1 μM; 24 h) significantly reduces MDA-MB-468 cell viability and reduces high molecular weight HSP90 complexes by disrupting epichaperome structure, while inducing decreased p-ERK phosphorylation levels and c-PARP cleavage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, ASPC1
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Concentration:1 μM
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Incubation Time:1 h
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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.
In Vivo
Icapamespib hydrochloride can target Alzheimer's disease and pedicled blastoma[2].
124I-labeled Icapamespib hydrochloride derivatives have been used to detect and quantify Epichaperomes in vivo by PET imaging[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (6-8 weeks old, 18-20 g) bearing U87MG glioblastoma xenografts[1]
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Dosage:10 mg/kg Icapamespib
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Administration:Intravenous injection via tail vein, twice weekly for 3 weeks.
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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.
- Neurotoxicity Study
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Pull-down
- Immunoprecipitation
- Protocol for Bimolecular Fluorescence Complementation (BiFC) Assay
- Breast Cancer Modeling
- Co-Immunoprecipitation
- Protocol for Yeast Two-Hybrid (Y2H) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Alzheimer’s Disease Modeling
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2267287-26-1
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Appearance Solid
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Masse moléculaire 599.32
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Formule C19H25Cl2IN6O2S
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Color White to off-white
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SMILES
IC1=C(SC2=NC3=C(N2CCNCC(C)(C)C)N=CN=C3N)C=C4OCOC4=C1.Cl.Cl
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Synonyms
PU-HZ151 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Environ Sci Technol
IodoFinder: Machine Learning-Guided Recognition of Iodinated Chemicals in Nontargeted LC-MS/MS Analysis. [Abstract]2025 Mar 11;59(9):4530-4539. PMID: 40015982
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (166.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 9.09 mg/mL (15.17 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bolaender A, et al. Chemical tools for epichaperome-mediated interactome dysfunctions of the central nervous system. Nat Commun. 2021;12(1):4669. Published 2021 Aug 3. [Content Brief]
[2]. Pasala C, et al. Epichaperomes: redefining chaperone biology and therapeutic strategies in complex diseases. RSC Chem Biol. 2025 Mar 19;6(5):678-698. [Content Brief]
[3]. Bay S, et al. Synthesis and Characterization of Click Chemical Probes for Single-Cell Resolution Detection of Epichaperomes in Neurodegenerative Disorders. Biomedicines. 2024 Jun 4;12(6):1252. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 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 | |
| DMSO | 20 mM | 0.0834 mL | 0.4171 mL | 0.8343 mL | 2.0857 mL |
| 25 mM | 0.0667 mL | 0.3337 mL | 0.6674 mL | 1.6686 mL | |
| 30 mM | 0.0556 mL | 0.2781 mL | 0.5562 mL | 1.3905 mL | |
| 40 mM | 0.0417 mL | 0.2086 mL | 0.4171 mL | 1.0428 mL | |
| 50 mM | 0.0334 mL | 0.1669 mL | 0.3337 mL | 0.8343 mL | |
| 60 mM | 0.0278 mL | 0.1390 mL | 0.2781 mL | 0.6952 mL | |
| 80 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.5214 mL | |
| 100 mM | 0.0167 mL | 0.0834 mL | 0.1669 mL | 0.4171 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Icapamespib hydrochloride Related Classifications
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