CAS NO: | 203258-38-2 |
包装: | 50mg, 100mg, 250mg |
规格: | ≥98% |
Brostallicin is a synthetic, alpha-bromoacrylic, second-generation minor groove binder (MGB), related to distamycin A, with potential antineoplastic activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this agent appears to bind covalently to DNA in a different manner and its activity does not depend on a functional DNA mismatch repair (MMR) mechanism. Accordingly, brostallicin may be effective against MMR-defective tumors that are refractory to various anticancer agents. References: 6. Bruckheimer, Elizabeth; Kiefer, Jeff; Mousses, Spyro; Shanmugam, Kandavel; Yin, Hongwei; Weitman, Steve. Target expression-based method for assessing sensitivity to brostallicin. PCT Int. Appl. (2009), 66pp. CODEN: PIXXD2 WO 2009126970 A1 20091015 CAN 15440645 AN 2009:1262339
纯度:≥98%
CAS:203258-38-2