Zelavespib hydrochloride
Based on 13 publication(s) in Google Scholar
Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
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- Pureté: 99.25%
- CAS No.: 2095432-24-7
- Formule: C18H22ClIN6O2S
- Masse moléculaire:548.83
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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)
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Publications Citing Use of MedChemExpress (MCE) Zelavespib hydrochloride
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
- Nat Commun. 2017 Sep 4;8(1):422. [Abstract]
- Theranostics. 2019 Aug 12;9(20):5769-5783. [Abstract]
- Theranostics. 2019 Jan 1;9(2):554-572. [Abstract]
- J Control Release. 2026 May 10:393:114828. [Abstract]
- Pharmacol Res. 2020 Jan;151:104512. [Abstract]
- Int J Biol Macromol. 2025 Dec 3;337(Pt 1):149421. [Abstract]
- Br J Pharmacol. 2021 Nov;178(22):4485-4500. [Abstract]
- Curr Issues Mol Biol. 2024 Mar 29;46(4):2946-2960. [Abstract]
- Curr Issues Mol Biol. 2023 Aug 23;45(9):7011-7026. [Abstract]
- Viruses. 2021 Apr 2;13(4):610. [Abstract]
- Authorea. April 10, 2021.
- bioRxiv. 2021 Jan 27.
Customer Validation & Images
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WB
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RT-PCR
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Cell Proliferation/Viability Assay
Activité biologique
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HSP90 51 nM (IC50, MDA-MB-468 cells) |
Zelavespib hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells. Zelavespib inhibits the growth of several tumor cells, such as MDA-MB-468, MDA-MB-231 and HCC-1806 cells, with IC50s of 65 ± 8 nM, 140 ± 5 nM and 87 ± 3 nM, respectively, and such inhibition is associated with a G2-M block arrest. Zelavespib (10-1000 nM) induces significant apoptosis in triple-negative breast cancers (TNBCs). Zelavespib (0.5, 1 μM) also downregulates oncoproteins involved in the invasive potential of TNBCs[1]. Zelavespib (0.5 μM) decreases and depletes the BCR signaling kinases. Zelavespib (0.25-10 μM) is cytotoxic to CLL cells but shows minimal effects on PBMC or resting B cells. In addition, Zelavespib (0-1 μM) reduces CLL viability via the induction of mitochondrial apoptosis, and antagonizes the survival signals from CLL microenvironment at 0.5 μM[2]. Zelavespib (0.05 μM) induces apoptosis of MDA-MB-231, BT-474, and MCF7 cells, and such induction is enhanced by TNF-α. Zelavespib (0.05 μM) degradates IKKβ, and down-regulates the NF-κB transcriptional activity induced by TNF-α treatment[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2095432-24-7
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Appearance Solid
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Masse moléculaire 548.83
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Formule C18H22ClIN6O2S
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Color Light yellow to yellow
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SMILES
CC(C)NCCCN1C(SC2=C(C=C3OCOC3=C2)I)=NC4=C(N=CN=C14)N.Cl
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Synonyms
PU-H71 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 (13)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286
Zelavespib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
Inoculation of THP-1 cells into 12-well cell culture plates and treated with indicated doses of Pimitespib, IPI-504, PU-H71 (0, 15, 30, 62.5, 125, 250, 500, 1000 nM), or STA-9090 for 18 h. SAMHD1 protein levels were analyzed by western blot.
Zelavespib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
RT-qPCR analysis of SAMHD1 mRNA levels in THP-1 cells treated with indicated concentrations of HSP90 inhibitors (IPI-504 (125, 250, 500 nM), PU-H71, or STA-9090) for 18 h.
Zelavespib hydrochloride purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
MTT assay measuring THP-1 cell viability after 18-hour treatment with PU-H71 (0, 125, 250, 500 nM).
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Nat Commun
2017 Sep 4;8(1):422. PMID: 28871086 -
Theranostics
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]2019 Aug 12;9(20):5769-5783. PMID: 31534518 -
Theranostics
2019 Jan 1;9(2):554-572. PMID: 30809293 -
J Control Release
The HSP90-dependent bioorthogonal PROTAC prodrug system enables tumor-selective and enhanced protein degradation. [Abstract]2026 May 10:393:114828. PMID: 41839264 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan;151:104512. PMID: 31726100 -
Int J Biol Macromol
17-AAG promotes the degradation of HSP90 client METTL3 to suppress MYC RNA m6A modification and expression in colorectal cancer. [Abstract]2025 Dec 3;337(Pt 1):149421. PMID: 41349747 -
Br J Pharmacol
Inhibition of heat shock protein (HSP) 90 reverses signal transducer and activator of transcription (STAT) 3-mediated muscle wasting in cancer cachexia mice. [Abstract]2021 Nov;178(22):4485-4500. PMID: 34265073 -
Curr Issues Mol Biol
FLT3 and IRAK4 Inhibitor Emavusertib in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]2024 Mar 29;46(4):2946-2960. PMID: 38666914 -
Curr Issues Mol Biol
HSP90 Inhibitor PU-H71 in Combination with BH3-Mimetics in the Treatment of Acute Myeloid Leukemia. [Abstract]2023 Aug 23;45(9):7011-7026. PMID: 37754227 -
Viruses
Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]2021 Apr 2;13(4):610. PMID: 33918368 -
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Solvant et solubilité
DMSO : 100 mg/mL (182.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.56 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 (4.56 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 14.29 mg/mL (26.04 mM); Clear solution; Need ultrasonic
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.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
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- Italian - IT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Caldas-Lopes E, et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc Natl Acad Sci U S A. 2009 May 19;106(20):8368-73. [Content Brief]
[2]. Guo A, et al. HSP90 stabilizes B-cell receptor kinases in a multi-client interactome: PU-H71 induces CLL apoptosis in a cytoprotective microenvironment. Oncogene. 2017 Jun 15;36(24):3441-3449. [Content Brief]
[3]. Qu Z, et al. PU-H71 effectively induces degradation of IκB kinase β in the presence of TNF-α. Mol Cell Biochem. 2014 Jan;386(1-2):135-42. [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 |
|---|---|---|---|---|---|
| DMSO | 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 | |
| 30 mM | 0.0607 mL | 0.3037 mL | 0.6074 mL | 1.5184 mL | |
| 40 mM | 0.0456 mL | 0.2278 mL | 0.4555 mL | 1.1388 mL | |
| 50 mM | 0.0364 mL | 0.1822 mL | 0.3644 mL | 0.9110 mL | |
| 60 mM | 0.0304 mL | 0.1518 mL | 0.3037 mL | 0.7592 mL | |
| 80 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5694 mL | |
| 100 mM | 0.0182 mL | 0.0911 mL | 0.1822 mL | 0.4555 mL |
Zelavespib hydrochloride Related Classifications
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