计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Daunorubicin HCl抑制DNA和RNA合成,抑制DNA合成时,Ki为0.02 μM。强效抗癌剂,已证明是 DNA 和 RNA 合成的强抑制剂。自发荧光的蒽环类抗生素,抗癌药。Pgp、MRP-1 和 BCRP 的底物。已利用荧光特性来测量药物外排泵活性,以及解?决许多重要问题,如多种多药耐药蛋白的胞内定位和亚细?胞器(高尔基体和溶酶体)在药物螯合中的作用及其在耐?药表型中的含义。根据 pH 分配型机理将柔红霉素螯合进溶酶体。DNA 和 RNA 合成的强抑制剂。A DNA intercalator which may suppress acute leukemia proliferation
Information
Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibitsDNAsynthesis withKiof 0.02 μM in a cell-free assay. Daunorubicin is atopoisomerase IIinhibitor that inducesapoptosis.
In vitro
At drug concentrations that reflect the peak plasma concentration after Daunorubicin administration, the primary mechanism is likely to be through interaction with topoisomerase II, which may be a primary triggering event for growth arrest and/or cell killing through a signalling pathway leading to apoptosis, at least in leukemic cells and thymocytes. The quinone structure permits daunorubicin to act as electron acceptors in reactions mediated by oxoreductive enzymes including cytochrome P450 reductase, NADH dehydrogenase, and xanthine oxidase. At Daunorubicin concentrations exceeding approximately 2–4 μM, free radical mediated toxicity and DNA cross-linking may become evident. Daunorubicin inhibits both DNA and RNA syntheses in HeLa cells over a concentration range of 0.2 through 2 μM. Daunorubicin inhibits both DNA syntheses in Ehrlich ascites tumor cells over a concentration range of 4 μM. Daunorubic triggers apoptosis at concentrations of 0.5 and 1 μM in either HL-60 or U-937 human leukemic cells. Daunorubicin stimulates ceramide elevation and apoptosis in P388 and U937 cells through de novo synthesis via activation of the enzyme ceramide synthase. Daunorubicin dose-dependently increases the phosphatidylserine exposure and consequent procoagulant activity of human umbilical vein endothelial cells. Daunorubicin (0.2 mM) significantly enhances the release of endothelial microparticles which are highly procoagulant in human umbilical vein endothelial cells.
In vivo
Cell Data
cell lines:
Concentrations:
Incubation Time:
Powder Purity:≥95%
H301: 吞咽会中毒
H341: 怀疑引起遗传缺陷
H351: 怀疑会致癌
H302: 吞食有害
H334: 吸入可能引起过敏或哮喘病症状或呼吸困难
H360: 可能对生育能力或胎儿造成伤害
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P321: 特殊处理(请参阅此标签上的...)。
P405: 密闭存放
P501: 将内容物/容器送到批准的废物处理厂处理
P264: 处理后要彻底洗手。
P284: 如果通风不良,请佩戴呼吸防护装置。
P281: 根据需要使用个人防护设备。
P270: 使用本产品时,请勿进食、饮水或吸烟。
P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。
P330: 漱口
P203: 使用前,获取、阅读并遵守所有安全说明。
P301+P316: 如果吞咽:立即寻求紧急医疗救助。
P301+P317: 如果被吞咽:请寻求医疗帮助。
P318: 如果暴露或担心,请就医。
P342+P316: 如果出现呼吸道症状:立即寻求急救。
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | D409068 |