Nimustine
Based on 1 publication(s) in Google Scholar
Nimustine 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 activates p38 MAPK/JNK signaling pathway, and exhibits 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。
- CAS 番号: 42471-28-3
- 分子式: C9H13ClN6O2
- 分子量:272.69
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Nimustine
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SF-126 | IC50 |
310 μM
Compound: ACNU
|
Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay in presence of O6-BG
Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay in presence of O6-BG
|
[PMID: 27041398] |
| SF-126 | IC50 |
320 μM
Compound: ACNU
|
Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay
Cytotoxicity against human SF126 cells expressing low level of AGT assessed as cell survival after 24 hrs by CCK8 assay
|
[PMID: 27041398] |
| SF-126 | IC50 |
360 μM
Compound: ACNU
|
Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability pretreated with O6-BG for 2 hrs followed by addition of compound measured after 24 hrs by CCK8 assay
Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability pretreated with O6-BG for 2 hrs followed by addition of compound measured after 24 hrs by CCK8 assay
|
[PMID: 28197307] |
| SF-126 | IC50 |
450 μM
Compound: ACNU
|
Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against AGT-deficient human SF126 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
|
[PMID: 28197307] |
| U-87MG ATCC | IC50 |
0.84 μM
Compound: Nimustine
|
Cytotoxicity against human U87MG cells after 72 hrs by MTT assay
Cytotoxicity against human U87MG cells after 72 hrs by MTT assay
|
[PMID: 20184290] |
体外実験
Nimustine (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. Further protocols information, click here.
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Cell Line:LN-229 cell line
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Concentration:50 μM
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Incubation Time:72-120 hours
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Result:Time-dependently induced apoptosis.
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Cell Line:LN-229
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Concentration:50 μM
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Incubation Time:24-120 hours
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Result:Increased the expressions of cleaved of bim and caspase-3/8/9.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C3H/HeN mice with solid FM3A tumors[2]
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Dosage:15 and 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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 42471-28-3
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分子量 272.69
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分子式 C9H13ClN6O2
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SMILES
O=C(NCC1=CN=C(C)N=C1N)N(CCCl)N=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
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
プロトコル
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
純度とドキュメンテーション
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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)