Ellipticine CAS: 519-23-3
MF: C17H14N2
MW: 246.31
A DNA intercalating inhibitor of Topo II.

Ellipticine (CAS 519-23-3)

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应用; A DNA intercalating inhibitor of Topo II
CAS号码: 519-23-3
纯度: ≥98%
分子量: 246.31
分子式: C17H14N2
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* 参考分析证明 大量特定数据 (包括水 含量).
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Ellipticine is a polyaromatic small molecule DNA intercalator, demonstrated to inhibit Topo II (DNA topoisomerase II) and to form covalent adducts with DNA. The formation of Ellipticine-DNA adducts is correlated to cytotoxicity and these adducts are suggested to interfere with DNA replication in the S phase. Antineoplastic effects are demonstrated with Ellipticine. Processing of Ellipticine by cytochrome p450 produces the adduct forming metabolites 13- and 12-hydroxyellipticine, and Ellipticine is described to inhibit cytochrome p450 CYP1A1 activity. Ellipticine was also shown to block p53 protein phosphorylation.


参考文献

1. Froelich-Ammon, S.J., et al. 1995. J. Biol. Chem. 270: 14998-15004. PMID: 7797481
2. Ohashi, M., et al. 1995. Jpn. J. Cancer Res. 86: 819-827. PMID: 7591958
3. Chang, C.Y. and Puga, A. 1998. Mol. Cell. Biol. 18: 525-535. PMID: 9418899
4. Poljaková, J., et al. 2009. Biochem. Pharmacol. 77: 1466-1479. PMID: 19426684

外观 :
Bright yellow solid
物理状态 :
Solid
溶解度 :
Soluble in DMSO, ethanol, and methanol. Insoluble in water.
保存 :
Store at 4° C
熔点 :
174.19° C (Predicted)
沸点 :
~495.4° C at 760 mmHg (Predicted)
密度 :
~1.3 g/cm3 (Predicted)
折射率 :
n20D 1.78
IC50 :
Breast carcinoma cells: IC50 = 0.1 µg/mL (Homo sapiens); Vero (Kidney cells): IC50 = 0.2 µg/mL (Chlorocebus aethiops); HIV-1: IC50 = 30.1 µM
pK值 :
pKb: 7.03
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
RTECS :
UU8825000
PubChem CID :
3213
默克索引 :
14: 3548
MDL 号码 :
MFCD00010524
EC号码 :
208-264-0
Beilstein 注册 :
221300
SMILES :
CC1=C2C(=C(C3=C1C=CN=C3)C)C4=CC=CC=C4N2

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PMID: # 27769881  Siebert, MN. et al. 2017. Comp. Biochem. Physiol. B, Biochem. Mol. Biol. 203: 115-121.

PMID: # 28623690  Siebert, MN. et al. 2017. Aquat. Toxicol. 189: 142-149.

PMID: # 28555524  Wen, HL. et al. 2017. Immunopharmacol Immunotoxicol. 39: 219-224.

PMID: # 28498409  Kumarasamy, VM. et al. 2017. Int. J. Oncol. 51: 145-157.

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