Zabadinostat
Based on 4 publication(s) in Google Scholar
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.83%
- CAS 番号: 934828-12-3
- 分子式: C24H29N5O
- 分子量:403.52
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Zabadinostat
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Customer Validation & Images
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RT-PCR
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Flow Cytometry
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WB
生物活性
製品説明
IC50 & Target
[1]|
HDAC1 63 nM (IC50) |
HDAC3 550 nM (IC50) |
HDAC2 570 nM (IC50) |
体外実験
Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
For Zabadinostat, after oral dosing in murine and canine models, peak plasma concentrations (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-Zabadinostat at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with Zabadinostat‐related material still present in tissue 21 days after the dose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 934828-12-3
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性状 Solid
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分子量 403.52
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分子式 C24H29N5O
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Color White to off-white
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SMILES
O=C(NC1=C(N)C=CC=C1)C2=CC=C(C3CCN(CC4=CN(C)N=C4C)CC3)C=C2
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別名
CXD101
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
2024 Oct 15;5(10):101770. PMID: 39368485 -
Cancer Immunol Immunother
HDAC1-3 inhibition triggers NEDD4-mediated CCR2 downregulation and attenuates immunosuppression in myeloid-derived suppressor cells. [Abstract]2025 Feb 1;74(3):81. PMID: 39891718
Zabadinostat purchased from MedChemExpress. Usage Cited in: Cancer Immunol Immunother. 2025 Feb 1;74(3):81. [Abstract]
Total RNA was extracted from in vitro M-MDSCs, and qRT-PCR was performed to measure the mRNA expression of Ccr2 treated with Zabadinostat (CXD101) (250 nM).
Zabadinostat purchased from MedChemExpress. Usage Cited in: Cancer Immunol Immunother. 2025 Feb 1;74(3):81. [Abstract]
Flow cytometry of CCR2 expression on in vitro M-MDSCs after 6 h of treatment with CXD101 (250 nM).
Zabadinostat purchased from MedChemExpress. Usage Cited in: Cancer Immunol Immunother. 2025 Feb 1;74(3):81. [Abstract]
In vitro MDSCs treated with CXD101 (250 nM), MG-132 (5 µM), or CXD101 and MG-132 for 6 h. The protein levels of NEDD4, CCR2, and ubiquitin were analyzed by western blot.
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溶剤 & 溶解度
体外:
DMSO : ≥ 31 mg/mL (76.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (6.20 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 (6.20 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.
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.
純度とドキュメンテーション
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データシート (272 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Eyre TA, et al. Predictive biomarkers for disease sensitivity in lymphoma - the holy grail for HDAC inhibitors? Oncotarget. 2018 Dec 18;9(99):37280-37281. [Content Brief]
[2]. Eyre TA, et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019 Jan 1;125(1):99-108. [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 | 2.4782 mL | 12.3910 mL | 24.7819 mL | 61.9548 mL |
| 5 mM | 0.4956 mL | 2.4782 mL | 4.9564 mL | 12.3910 mL | |
| 10 mM | 0.2478 mL | 1.2391 mL | 2.4782 mL | 6.1955 mL | |
| 15 mM | 0.1652 mL | 0.8261 mL | 1.6521 mL | 4.1303 mL | |
| 20 mM | 0.1239 mL | 0.6195 mL | 1.2391 mL | 3.0977 mL | |
| 25 mM | 0.0991 mL | 0.4956 mL | 0.9913 mL | 2.4782 mL | |
| 30 mM | 0.0826 mL | 0.4130 mL | 0.8261 mL | 2.0652 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6195 mL | 1.5489 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2391 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4130 mL | 1.0326 mL |
Zabadinostat 関連分類
HY-100748 関連分類
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