Debio 0932
Based on 6 publication(s) in Google Scholar
Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.76%
- CAS. Nr.: 1061318-81-7
- Formel: C22H30N6O2S
- Molecular Weight:442.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Debio 0932
More
Biologische Aktivität
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HSP90α 100 nM (IC50) |
HSP90β 103 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
100 nM
Compound: 19; CUDC-305
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Antiproliferative activity against human MV4-11 cells after 120 hrs by TopCount scintillation analysis
Antiproliferative activity against human MV4-11 cells after 120 hrs by TopCount scintillation analysis
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[PMID: 31663736] |
Debio 0932 is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively. Debio 0932 (CUDC-305) binds to the tumor HSP90 complex with a mean IC50 of 48.8 nM. Debio 0932 (1 μM) promotes degradation of multiple HSP90 client proteins in cancer cell lines. Debio 0932 also shows inhibitory activities against the proliferation of 40 cancer cell lines (containing 34 solid and 6 hematologic tumor-derived lines) with an IC50 ranging from 40 to 900 nM (mean IC50, 220 nM)[1]. Debio 0932 strongly binds to cancer-derived HSP90 complex with an IC50 of 61.2 nM in H1975 cells and 74.2 nM in H1993 cells, respectively. Debio 0932 (CUDC-305, 1 μM) durably induces oncoprotein degradation in NSCLC cell lines with mutations that can confer resistance to erlotinib[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1061318-81-7
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Appearance Solid
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Molecular Weight 442.58
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Formel C22H30N6O2S
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Color White to yellow
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SMILES
NC1=NC=CC2=C1N=C(SC3=C(N(C)C)C=C(OCO4)C4=C3)N2CCNCC(C)(C)C
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Synonyms
CUDC-305
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Clin Transl Med
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology. [Abstract]2022 Jul;12(7):e961. PMID: 35839307 -
EMBO Mol Med
A clinically compatible drug-screening platform based on organotypic cultures identifies vulnerabilities to prevent and treat brain metastasis. [Abstract]2022 Mar 7;14(3):e14552. PMID: 35174975 -
Br J Cancer
Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma. [Abstract]2023 May;128(10):1941-1954. PMID: 36959380 -
Cell Rep Methods
Cortical organoid-derived models of the melanoma brain metastatic niche enable prioritization of cancer-targeting drugs. [Abstract]2025 Dec 15;5(12):101236. PMID: 41240911 -
PLoS One
The heat shock protein 90 inhibitor RGRN-305 attenuates SARS-CoV-2 spike protein-induced inflammation in vitro but lacks effectiveness as COVID-19 treatment in mice. [Abstract]2024 Sep 26;19(9):e0310915. PMID: 39325762 -
Lösungsmittel & Löslichkeit
DMSO : 75 mg/mL (169.46 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.65 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 (5.65 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.
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.
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.
Protokoll
Human cancer cell lines are plated at 5,000 to 10,000 per well in 96-well plates with culture medium. The cells are then incubated with compounds (Debio 0932) at various concentrations for 120 h. Growth inhibition is assessed by ATP content assay using the ATPlite kit. Briefly, a 25-μL cell lysis solution is added to the 50-μL phenol red-free culture medium per well to lyse cells and stabilize ATP. Then 25-μL substrate solutions are added to the wells, and subsequently, luminescence is measured with a TopCount liquid scintillation analyzer. Values are expressed as a percentage relative to those obtained in untreated controls. IC50 values are calculated using PRISM software with sigmoidal dose-response curve fitting[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
When tumors are established after implantation, animals with proper tumor size are randomly assigned into different groups. Debio 0932 is formulated in 30% Captisol and delivered by oral gavage based on the body weight of each individual animal. The control group is treated with vehicle (30% Captisol) using the same dosing paradigm. In combination studies, paclitaxel or camptothecin-11 is diluted in 0.9% normal saline and injected i.p. twice weekly[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[1]. Bao R, et al. CUDC-305, a novel synthetic HSP90 inhibitor with unique pharmacologic properties for cancer therapy. Clin Cancer Res. 2009 Jun 15;15(12):4046-57. [Content Brief]
[2]. Stenderup K, et al. Debio 0932, a new oral Hsp90 inhibitor, alleviates psoriasis in a xenograft transplantation model. Acta Derm Venereol. 2014 Nov;94(6):672-6. [Content Brief]
[3]. Bao R, et al. Targeting heat shock protein 90 with CUDC-305 overcomes erlotinib resistance in non-small cell lung cancer. Mol Cancer Ther. 2009 Dec;8(12):3296-306. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2595 mL | 11.2974 mL | 22.5948 mL | 56.4870 mL |
| 5 mM | 0.4519 mL | 2.2595 mL | 4.5190 mL | 11.2974 mL | |
| 10 mM | 0.2259 mL | 1.1297 mL | 2.2595 mL | 5.6487 mL | |
| 15 mM | 0.1506 mL | 0.7532 mL | 1.5063 mL | 3.7658 mL | |
| 20 mM | 0.1130 mL | 0.5649 mL | 1.1297 mL | 2.8243 mL | |
| 25 mM | 0.0904 mL | 0.4519 mL | 0.9038 mL | 2.2595 mL | |
| 30 mM | 0.0753 mL | 0.3766 mL | 0.7532 mL | 1.8829 mL | |
| 40 mM | 0.0565 mL | 0.2824 mL | 0.5649 mL | 1.4122 mL | |
| 50 mM | 0.0452 mL | 0.2259 mL | 0.4519 mL | 1.1297 mL | |
| 60 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9414 mL | |
| 80 mM | 0.0282 mL | 0.1412 mL | 0.2824 mL | 0.7061 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2259 mL | 0.5649 mL |
Debio 0932 Related Classifications
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