9-Hydroxyellipticin
9-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice.
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: 51131-85-2
- 分子式: C17H14N2O
- 分子量:262.31
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Topoisomerase アイソフォーム固有の製品をすべて表示
More
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | ED50 |
0.08 μM
Compound: 19b
|
The effective dose against L1210 cell growth
The effective dose against L1210 cell growth
|
[PMID: 4009597] |
| NCI-H358 | IC50 |
5.6 μM
Compound: 2 (9-OH-ellipticin)
|
Cytotoxicity against H 358 human lung cancer cell line
Cytotoxicity against H 358 human lung cancer cell line
|
[PMID: 1479585] |
| NCI-H417 | IC50 |
3.5 μM
Compound: 2 (9-OH-ellipticin)
|
Cytotoxicity against N 417 human lung cancer cell line
Cytotoxicity against N 417 human lung cancer cell line
|
[PMID: 1479585] |
| NCI-H460 | IC50 |
2.6 μM
Compound: 2 (9-OH-ellipticin)
|
Cytotoxicity against H 460 human lung cancer cell line
Cytotoxicity against H 460 human lung cancer cell line
|
[PMID: 1479585] |
| NCI-H69 | IC50 |
1.7 μM
Compound: 2 (9-OH-ellipticin)
|
Cytotoxicity against H69 human lung cancer cell line
Cytotoxicity against H69 human lung cancer cell line
|
[PMID: 1479585] |
| NIH3T3 | IC50 |
0.9 μM
Compound: 4
|
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 28063783] |
| Sarcoma-180 | IC50 |
0.44 μM
Compound: 4
|
Cytotoxicity against mouse Sarcoma 180 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against mouse Sarcoma 180 cells assessed as reduction in cell viability after 72 hrs by MTT assay
|
[PMID: 28063783] |
化学情報
-
CAS 番号 51131-85-2
-
分子量 262.31
-
分子式 C17H14N2O
-
SMILES
OC1=CC2=C(NC3=C2C(C)=C(C=NC=C4)C4=C3C)C=C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Renault G, et al. In vivo exposure to four ellipticine derivatives with topoisomerase inhibitory activity results in chromosome clumping and sister chromatid exchange in murine bone marrow cells. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):281-6. [Content Brief]
[2]. Saeki K, et al. Cardioprotective effects of 9-hydroxyellipticine on ischemia and reperfusion in isolated rat heart. Jpn J Pharmacol. 2002 May;89(1):21-8. [Content Brief]
[3]. G Renault, et al. In vivo exposure to four ellipticine derivatives with topoisomerase inhibitory activity results in chromosome clumping and sister chromatid exchange in murine bone marrow cells. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):281-6. [Content Brief]
[4]. Le Pecq JB, et al. A new antitumoral agent: 9-hydroxyellipticine. Possibility of a rational design of anticancerous drugs in the series of DNA intercalating drugs. Proc Natl Acad Sci U S A. 1974 Dec;71(12):5078-82. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)