Elinafide
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Elinafide is an anticancer agent with a naphthalimide structure that targets DNA. Elinafide interferes with cell metabolism by inserting a planar ring into the DNA double helix and interacting with enzymes through its side chain.LU-79553 is a DNA-binding topoisomerase II inhibitor. The IC50 value of Elinafide for HT-29 cells is 0.014 μM.
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: 98.02%
- CAS 番号: 162706-37-8
- 分子式: C31H28N4O4
- 分子量:520.58
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Topoisomerase アイソフォーム固有の製品をすべて表示
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生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.07 μM
Compound: Elinafide
|
In vitro concentration required to reduce cell number to 50% in human cervical carcinoma (HeLa) culture
In vitro concentration required to reduce cell number to 50% in human cervical carcinoma (HeLa) culture
|
[PMID: 12477366] |
| HeLa | IC50 |
0.07 μM
Compound: Elinafide
|
In vitro cytotoxicity against human cervical carcinoma (HeLa) cell line
In vitro cytotoxicity against human cervical carcinoma (HeLa) cell line
|
[PMID: 14998328] |
| HeLa | IC50 |
0.07 μM
Compound: elinafide
|
Growth inhibitory concentration against human cervical carcinoma (HeLa) cell line
Growth inhibitory concentration against human cervical carcinoma (HeLa) cell line
|
[PMID: 15084122] |
| HT-29 | IC50 |
0.014 μM
Compound: LU-79553
|
In vitro cytotoxicity against HT-29 (human colon adenocarcinoma) cell line.
In vitro cytotoxicity against HT-29 (human colon adenocarcinoma) cell line.
|
[PMID: 9046334] |
| HT-29 | IC50 |
0.017 μM
Compound: Elinafide
|
In vitro concentration required to reduce cell number to 50% in human colon carcinoma (HT-29) culture
In vitro concentration required to reduce cell number to 50% in human colon carcinoma (HT-29) culture
|
[PMID: 12477366] |
| HT-29 | IC50 |
0.017 μM
Compound: Elinafide
|
In vitro cytotoxicity against human colon carcinoma (HT-29) cell line
In vitro cytotoxicity against human colon carcinoma (HT-29) cell line
|
[PMID: 14998328] |
| HT-29 | IC50 |
0.017 μM
Compound: elinafide
|
Growth inhibitory concentration against human colon adenocarcinoma cell line (HT-29)
Growth inhibitory concentration against human colon adenocarcinoma cell line (HT-29)
|
[PMID: 15084122] |
| HT-29 | IC50 |
0.038 μM
Compound: elinafide
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 19058969] |
| HT-29 | IC50 |
0.15 nM
Compound: 2, LU-79553
|
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in HT-29 (human colon)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in HT-29 (human colon)
|
[PMID: 11311063] |
| Lewis lung carcinoma cell line | IC50 |
11 nM
Compound: 2, LU-79553
|
Inhibitory concentration required to reduce cell number to 50% of control cultures in LL(Lewis lung carcinoma cell line)
Inhibitory concentration required to reduce cell number to 50% of control cultures in LL(Lewis lung carcinoma cell line)
|
[PMID: 11311063] |
| MDA-MB-231 | IC50 |
0.06 μM
Compound: 3 (LU-79553)
|
Inhibition of human breast cancer cell line MDA-MB-231 growth
Inhibition of human breast cancer cell line MDA-MB-231 growth
|
[PMID: 11965367] |
| MOLT-4 | IC50 |
0.037 nM
Compound: 2, LU-79553
|
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in MOLT-4 (human leukemia)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in MOLT-4 (human leukemia)
|
[PMID: 11311063] |
| NCI-H460 | IC50 |
0.008 μM
Compound: 4
|
Cytotoxicity against human NCI-H460 cells after 3 days by cell counting analysis
Cytotoxicity against human NCI-H460 cells after 3 days by cell counting analysis
|
[PMID: 21880496] |
| P388 | IC50 |
1.5 nM
Compound: 2, LU-79553
|
Inhibitory concentration required to reduce cell number to 50% of control cultures in P388 (murine leukemia cell line)
Inhibitory concentration required to reduce cell number to 50% of control cultures in P388 (murine leukemia cell line)
|
[PMID: 11311063] |
| PC-3 | IC50 |
0.07 μM
Compound: 3 (LU-79553)
|
Inhibition of human prostate cancer cell line PC-3 growth
Inhibition of human prostate cancer cell line PC-3 growth
|
[PMID: 11965367] |
| PC-3 | IC50 |
0.32 μM
Compound: Elinafide
|
In vitro concentration required to reduce cell number to 50% in human postrate carcinoma (PC-3) culture
In vitro concentration required to reduce cell number to 50% in human postrate carcinoma (PC-3) culture
|
[PMID: 12477366] |
| PC-3 | IC50 |
0.32 μM
Compound: Elinafide
|
In vitro cytotoxicity against human prostate carcinoma (PC-3) cell line
In vitro cytotoxicity against human prostate carcinoma (PC-3) cell line
|
[PMID: 14998328] |
| PC-3 | IC50 |
0.32 μM
Compound: elinafide
|
Growth inhibitory concentration against human prostate carcinoma (PC-3) cell line
Growth inhibitory concentration against human prostate carcinoma (PC-3) cell line
|
[PMID: 15084122] |
| U-937 | IC50 |
0.34 nM
Compound: 2, LU-79553
|
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in U937 (human leukemia)
Inhibitory concentration of the drug resulting in inhibition of cell growth to 50% of controls in U937 (human leukemia)
|
[PMID: 11311063] |
化学情報
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CAS 番号 162706-37-8
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性状 Solid
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分子量 520.58
-
分子式 C31H28N4O4
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Color Light yellow to yellow
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SMILES
O=C1N(CCNCCCNCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O)C(C5=CC=CC6=CC=CC1=C56)=O
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別名
LU 79553
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 5 mg/mL (9.60 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
純度とドキュメンテーション
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データシート (271 KB)
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SDS (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Braña MF, et al. Naphthalimides as anti-cancer agents: synthesis and biological activity. Curr Med Chem Anticancer Agents. 2001;1(3):237-255. [Content Brief]
[2]. J Gallego, et al. Solution structure and dynamics of a complex between DNA and the antitumor bisnaphthalimide LU-79553: intercalated ring flipping on the millisecond time scale. Biochemistry. 1999 Nov 16;38(46):15104-15. [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. 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 | 1.9209 mL | 9.6047 mL | 19.2093 mL | 48.0234 mL |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL | 9.6047 mL |