Bizelesin  (Synonyms: NSC 615291; U-77779)

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].

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

815.70

C₄₃H₃₆Cl₂N₈O₅

129655-21-6

固体

Off-white to gray

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [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.   [Content Brief]

  [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.   [Content Brief]