Celiptium, also known as elliptinium acetate, a topoisomerase II inhibitor, is the acetate salt of elliptinium, a derivative of the alkaloid ellipticine isolated from species of the plant family Apocynaceae, including Bleekeria vitensis, a plant with anti-cancer properties. As a topoisomerase II inhibitor and intercalating agent, elliptinium stabilizes the cleavable complex of topoisomerase II and induces DNA breakages, thereby inhibiting DNA replication and RNA and protein synthesis.
CAS 58337-35-2 MFCD00866541
化学结构图
SMILES: CC(=O)[O-].Cc1c2cc[n+](C)cc2c(C)c2c1[nH]c1ccc(O)cc12
化学属性
| Mol. Formula | C18H17N2O.C2H3O2 |
|---|---|
| Mol. Weight | 336.38 |
| Appearance | solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | Celiptium, also known as elliptinium acetate, a topoisomerase II inhibitor, is the acetate salt of elliptinium, a derivative of the alkaloid ellipticine isolated from species of the plant family Apocynaceae, including Bleekeria vitensis, a plant with anti-cancer properties. As a topoisomerase II inhibitor and intercalating agent, elliptinium stabilizes the cleavable complex of topoisomerase II and induces DNA breakages, thereby inhibiting DNA replication and RNA and protein synthesis. |
|---|---|
| Synonym | Celiptium Ellipticine acetomethylate Elliptinium Elliptinium acetate N2-Methylhydroxyellipticinium acetate ellipticine acetate Elliptinium acetate; Celiptium; 9HME; HME; NMHE |
| CAS Number | 58337-35-2 |
| Formula | C20H20N2O3 |
| IUPAC Name | 9-hydroxy-2,5,11-trimethyl-6H-pyrido[4,3-b]carbazol-2-ium acetate |
| InChIKey | BOMZMNZEXMAQQW-UHFFFAOYSA-N |
| InChI | InChI=1S/C18H16N2O.C2H4O2/c1-10-15-9-20(3)7-6-13(15)11(2)18-17(10)14-8-12(21)4-5-16(14)19-18;1-2(3)4/h4-9,21H,1-3H3;1H3,(H,3,4) |
| Canonical SMILES | CC1=C2C(NC3=C2C=C(O)C=C3)=C(C)C4=CC=[N+](C)C=C41.CC([O-])=O |
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- Celiptium, also known as elliptinium acetate, a topoisomerase II inhibitor, is the acetate salt of elliptinium, a derivative of the alkaloid ellipticine isolated from species of the plant family Apocynaceae, including Bleekeria vitensis, a plant with anti-cancer properties. As a topoisomerase II inhibitor and intercalating agent, elliptinium stabilizes the cleavable complex of topoisomerase II and induces DNA breakages, thereby inhibiting DNA replication and RNA and protein synthesis.
安全信息
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 33 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 47,6254,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 18 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 47,6254,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 8 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 47,6254,1987
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 10200 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0209511
TYPE OF TEST : Micronucleus test ROUTE OF EXPOSURE : Intraperitoneal TEST SYSTEM : Rodent - mouse DOSE/DURATION : 10 mg/kg REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 89,281,1987
TYPE OF TEST : Sister chromatid exchange ROUTE OF EXPOSURE : Intraperitoneal TEST SYSTEM : Rodent - mouse DOSE/DURATION : 10 mg/kg REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 89,281,1987
TYPE OF TEST : DNA damage TEST SYSTEM : Human Cells - not otherwise specified DOSE/DURATION : 5 umol/L REFERENCE : BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 38,2077,1989
TYPE OF TEST : DNA inhibition TEST SYSTEM : Rodent - mouse Leukocyte DOSE/DURATION : 27 umol/L REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 47,6254,1987
