Bizelesin

Modify Date: 2024-01-09 15:35:38

Bizelesin Structure
Bizelesin structure
Common Name Bizelesin
CAS Number 129655-21-6 Molecular Weight 815.70300
Density 1.604g/cm3 Boiling Point N/A
Molecular Formula C43H36Cl2N8O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Bizelesin


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].

 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
Synonym More Synonyms

 Bizelesin Biological Activity

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].
Related Catalog
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]。
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.   

 Chemical & Physical Properties

Density 1.604g/cm3
Molecular Formula C43H36Cl2N8O5
Molecular Weight 815.70300
Exact Mass 814.21900
PSA 185.37000
LogP 9.52540
Index of Refraction 1.856

 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)