Nimustine hydrochloride
Based on 1 publication(s) in Google Scholar
Nimustine hydrochloride (ACNU) is the hydrochloride salt form of Nimustine (HY-13703). Nimustine hydrochloride is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNA damage response (DDR) signaling pathway. Nimustine hydrochloride activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity.
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- 純度: 99.00%
- CAS 番号: 55661-38-6
- 分子式: C9H14Cl2N6O2
- 分子量:309.15
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
MedChemExpress(MCE)の使用を引用している文献 Nimustine hydrochloride
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-87MG ATCC | IC50 |
0.72 μM
Compound: ACNU
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Cytotoxicity against human U87MG cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human U87MG cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 23992864] |
Nimustine hydrochloride (50 μM, 72 h) activates caspase and AP-1, upregulates the expression of bim, promotes the phosphorylation of c-Jun, and induces apoptosis in cell LN-229[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LN-229
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Concentration:50 μM
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Incubation Time:72 h
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Result:Increased the expressions of cleaved of bim and caspase-3/8/9.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeN mouse models[2]
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Dosage:15-30 mg/kg
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Administration:iv, every two weeks for 2 doses (30 mg/kg), or once weekly for 4 doses (15 mg/kg)
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Result:Inhibited tumor growth. Caused weight loss and white blood cell (WBC) depression.
化学情報
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CAS 番号 55661-38-6
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性状 Solid
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分子量 309.15
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分子式 C9H14Cl2N6O2
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Color White to off-white
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SMILES
O=C(NCC1=CN=C(C)N=C1N)N(CCCl)N=O.[H]Cl
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別名
ACNU
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Appl Mater Interfaces
Multi-Inlet Spheroid Generator for High-Throughput Combinatorial Drug Screening Based on the Tumor Microenvironment. [Abstract]2023 Jul 12;15(27):32087-32098. PMID: 37234040
溶剤 & 溶解度
DMSO : 62.5 mg/mL (202.17 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 and light). 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.08 mg/mL (6.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (275 KB)
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SDS (641 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Tomicic MT, et al. Apoptosis induced by temozolomide and nimustine in glioblastoma cells is supported by JNK/c-Jun-mediated induction of the BH3-only protein BIM. Oncotarget. 2015 Oct 20;6(32):33755-68. [Content Brief]
[2]. Shimizu F, et al. Effects of combined treatment with nimustine hydrochloride and radiation on solid FM3A tumor in mice. Jpn J Cancer Res. 1987 Jul;78(7):756-62. [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 and light). 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 | 3.2347 mL | 16.1734 mL | 32.3468 mL | 80.8669 mL |
| 5 mM | 0.6469 mL | 3.2347 mL | 6.4694 mL | 16.1734 mL | |
| 10 mM | 0.3235 mL | 1.6173 mL | 3.2347 mL | 8.0867 mL | |
| 15 mM | 0.2156 mL | 1.0782 mL | 2.1565 mL | 5.3911 mL | |
| 20 mM | 0.1617 mL | 0.8087 mL | 1.6173 mL | 4.0433 mL | |
| 25 mM | 0.1294 mL | 0.6469 mL | 1.2939 mL | 3.2347 mL | |
| 30 mM | 0.1078 mL | 0.5391 mL | 1.0782 mL | 2.6956 mL | |
| 40 mM | 0.0809 mL | 0.4043 mL | 0.8087 mL | 2.0217 mL | |
| 50 mM | 0.0647 mL | 0.3235 mL | 0.6469 mL | 1.6173 mL | |
| 60 mM | 0.0539 mL | 0.2696 mL | 0.5391 mL | 1.3478 mL | |
| 80 mM | 0.0404 mL | 0.2022 mL | 0.4043 mL | 1.0108 mL | |
| 100 mM | 0.0323 mL | 0.1617 mL | 0.3235 mL | 0.8087 mL |