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| | Nsc264136 Basic information |
| Product Name: | Nsc264136 | | Synonyms: | Nsc264136;9-Hydroxyellipticine, Hydrochloride;9-hydroxyellipticine HCl salt;5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol hydrochloride;9Hydroxyellipticine hydrochloride,9 Hydroxyellipticine hydrochloride | | CAS: | 52238-35-4 | | MF: | C17H15ClN2O | | MW: | 298.7668 | | EINECS: | | | Product Categories: | Other Enzyme Inhibitors and Activators. | | Mol File: | 52238-35-4.mol |  |
| | Nsc264136 Chemical Properties |
| Melting point | >223oC (dec.) | | storage temp. | Hygroscopic, -20°C Freezer, Under inert atmosphere | | solubility | DMSO (Slightly, Heated), Methanol (Slightly, Sonicated) | | form | Solid | | color | Orange to Dark Orange |
| | Nsc264136 Usage And Synthesis |
| Description | 9-Hydroxyellipticine is a derivative of ellipticine with diverse biological activities. It inhibits aroclor-induced activation of aniline hydroxylase, aminopyrine N-demethylase, and 7-ethoxycourmarin O-deethylase in rat liver microsomes (Kis = 3.5, 0.6, and 0.74 μM, respectively). 9-Hydroxyellipticine inhibits the growth of L1210 murine leukemia cells (IC50 = 3 nM) in vitro and increases survival in an L1210 mouse leukemia model. It inhibits carrageenan-induced edema and UV-induced erythema in guinea pigs. | | Uses | 9-Hydroxyellipticine Hydrochloride is a potent topoisomerase II inhibitor. | | in vivo | 9-Hydroxyellipticine (5 or 10 mg/kg, ip) results in chromosome clumping and sister chromatid exchange in murine bone marrow cells[1].
| Animal Model: | Three- to five-month-old C57B1/6 male mice[1]. | | Dosage: | 5 or 10 mg/kg. | | Administration: | IP. | | Result: | Resulted in chromosome clumping, chromatid aberrations, and micronuclei formation in murine bone marrow cells. |
| | IC 50 | Topoisomerase II | | References | [1] PIERRE LESCA . A class of strong inhibitors of microsomal monooxygenases: The elupticines[J]. Chemico-Biological Interactions, 1979, 24 2: Pages 189-197. DOI: 10.1016/0009-2797(79)90007-3
[2] M MONNOT. DNA-drug recognition and effects on topoisomerase II-mediated cytotoxicity. A three-mode binding model for ellipticine derivatives.[J]. The Journal of Biological Chemistry, 1991, 266 3: 1820-1829.
[3] J B LE PECQ. Antitumor activity of 9-hydroxyellipticine (NSC 210717) ON L1210 mouse leukemia and the effect of route of injection.[J]. Cancer research, 1976, 36 9 pt.1: 3067-3076.
[4] J CROS N D X A Thibault. [Anti-inflammatory effect of hydroxy-9-ellipticine].[J]. Comptes rendus hebdomadaires des seances de l’Academie des sciences. Serie D: Sciences naturelles, 1975, 281 15: 1139-1142.
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| | Nsc264136 Preparation Products And Raw materials |
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