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.
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- CAS No.: 51131-85-2
- 화학식: C17H14N2O
- 분자량:262.31
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
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Biological Activity
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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] |
Chemical Information
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CAS No. 51131-85-2
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분자량 262.31
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화학식 C17H14N2O
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SMILES
OC1=CC2=C(NC3=C2C(C)=C(C=NC=C4)C4=C3C)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)