Bioactivity | 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]. |
Invitro | 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,具有潜在的癌症处理潜力[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]。 |
Name | Bizelesin |
CAS | 129655-21-6 |
Formula | C43H36Cl2N8O5 |
Molar Mass | 815.70 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |