51131-85-2

• 常用中文名：9-hydroxyellipticine
• 常用英文名：9-hydroxyellipticine
• CAS号：51131-85-2
• 分子式：C₁₇H₁₄N₂O
• 分子量：262.30600
• 发布时间：2016-08-22 09:32:10
• 更新时间：2024-01-02 11:18:23
• 9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines.

名称

• 英文名: 5,11-dimethyl-6H-pyrido[4,3-b]carbazol-9-ol
• 英文别名: ELLIPTICINE,9-HYDROXY; 9-Hydroxyellipticin; 9-Hydroxyellipticine; EINECS 257-000-0; 9-hydroxyelipticine; IGIG 929; Hydroxyellipticine

物化性质

• 密度: 1.349g/cm3
• 沸点: 557.7ºC at 760mmHg
• 分子式: C₁₇H₁₄N₂O
• 分子量: 262.30600
• 闪点: 291.1ºC
• 精确质量: 262.11100
• PSA: 48.91000
• LogP: 4.19170

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UU8886500 CHEMICAL NAME : 6H-Pyrido(4,3-b)carbazol-9-ol, 5,11-dimethyl- CAS REGISTRY NUMBER : 51131-85-2 LAST UPDATED : 199410 DATA ITEMS CITED : 16 MOLECULAR FORMULA : C17-H14-N2-O MOLECULAR WEIGHT : 262.33 WISWESSER LINE NOTATION : T D6 B656 FM KMJ C1 J1 OQ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 50 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 102 mg/kg TOXIC EFFECTS : Behavioral - changes in motor activity (specific assay) Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - body temperature decrease TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 55 mg/kg/11D-I TOXIC EFFECTS : Blood - leukopenia Related to Chronic Data - death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 30 mg/kg SEX/DURATION : female 10 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - musculoskeletal system TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 20 mg/kg SEX/DURATION : female 9 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 20 mg/kg SEX/DURATION : female 8 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 10 mg/kg SEX/DURATION : female 8 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) TYPE OF TEST : Micronucleus test TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sister chromatid exchange MUTATION DATA TYPE OF TEST : Mutation in mammalian somatic cells TEST SYSTEM : Rodent - hamster Ovary DOSE/DURATION : 1 ug/L REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,3544,1983

合成路线

10371-86-5 ~67% 51131-85-2

文献：Anderson, Wayne K.; Gopalsamy, Ariamala; Reddy, Peech S. Journal of Medicinal Chemistry, 1994 , vol. 37, # 13 p. 1955 - 1963

115552-64-2 ~93% 51131-85-2

文献：Plug; Koomen; Pandit Synthesis, 1992 , # 12 p. 1221 - 1222

76004-29-0 ~93% 51131-85-2

文献：Pautet; Formisyn; Bourgois Archiv der Pharmazie, 1993 , vol. 326, # 8 p. 499 - 500

519-23-3 ~% 51131-85-2

文献：Plug; Koomen; Pandit Synthesis, 1992 , # 12 p. 1221 - 1222

上下游产品

上游产品  4
10371-86-5 115552-64-2 76004-29-0 519-23-3
下游产品  3
76004-29-0 102353-63-9 86542-48-5