Delanzomib (CEP-18770)
商品编号:
TS0515
备注:
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详细介绍
l 基本信息 |
产品名称 | Delanzomib |
一般描述 | Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. |
别 称 | CEP-18770 |
纯 度 | ≥98.0%(HPLC) | CAS NO. | 847499-27-8 |
分子式 | C21H28BN3O5 | 分子量 | 413.281 |
适用范围 | 生物试剂,适用于细胞培养等 |
l 理化信息 |
外 观 | 白色或类白色至浅棕色固体 |
溶解性(25°C) | DMSO | ≥50mg/ml |
乙醇 | ≥50mg/ml |
水 | Very slightly soluble |
l 生物学信息 |
生物活性/药理作用 | Delanzomib is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Delanzomib represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the tranion factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and tranional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory tranion factor NF-kappaB. |
l 存储 |
存储温度 | -20°C |
l 注意事项及免责声明 |
本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。 |
l 参考文献 |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |