Introduction:Basic information about CAS 129655-21-6|Bizelesin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Bizelesin |
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| CAS Number | 129655-21-6 | Molecular Weight | 815.70300 |
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| Density | 1.604g/cm3 | Boiling Point | / |
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| Molecular Formula | C43H36Cl2N8O5 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | 1,3-bis[2-[(8S)-8-(chloromethyl)-4-hydroxy-1-methyl-7,8-dihydro-3H-pyrrolo[3,2-e]indole-6-carbonyl]-1H-indol-5-yl]urea |
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| Synonym | More Synonyms |
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Bizelesin BiologicalActivity
| Description | Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity[1]. |
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| Related Catalog | Research Areas >>CancerSignaling Pathways >>Cell Cycle/DNA Damage >>DNA Alkylator/Crosslinker |
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| In Vitro | Bizelesin (0-5 μM, 4 h)可以通过靶向人类癌细胞 CEM 细胞中富含 AT的 DNA 域,造成 DNA 特异性损伤,进而造成癌细胞损伤,具有潜在的癌症治疗潜力[1]。 Bizelesin (0-500 nM)在 BSC-1 细胞中,当浓度为 10 nM 时导致 50% 的 DNA 合成抑制,相比之下,浓度为 160 nM 时才抑制 50% RNA 合成,而浓度高达至 200 nM 时也没有观察到蛋白质合成的抑制[2]。 |
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| References | [1]. J M Woynarowski, et al. AT-rich islands in genomic DNA as a novel target for AT-specific DNA-reactive antitumor drugs. J Biol Chem. 2001 Nov 2;276(44):40555-66. [2]. J M Woynarowski, et al. Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on replication of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta. 1997 Jul 17;1353(1):50-60. |
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Chemical & Physical Properties
| Density | 1.604g/cm3 |
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| Molecular Formula | C43H36Cl2N8O5 |
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| Molecular Weight | 815.70300 |
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| Exact Mass | 814.21900 |
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| PSA | 185.37000 |
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| LogP | 9.52540 |
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| Index of Refraction | 1.856 |
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| InChIKey | FONKWHRXTPJODV-UHFFFAOYSA-N |
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| SMILES | Cc1c[nH]c2c(O)cc3c(c12)C(CCl)CN3C(=O)c1cc2cc(NC(=O)Nc3ccc4[nH]c(C(=O)N5CC(CCl)c6c5cc(O)c5[nH]cc(C)c65)cc4c3)ccc2[nH]1 |
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Synonyms
| Benzo(1,2-b:4,3-b')dipyrrol-4-ol,6,6'-(carbonylbis(imino-1H-indole-5,2-diylcarbonyl))bis(8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-,(S-(R*,R*)) |
| U-77,779 |
| BIZELESIN |
| Bizelesin (USAN/INN) |