奈莫柔比星
中文名称 | 奈莫柔比星 |
---|---|
中文同义词 | 柰莫柔比星;奈莫柔比星;莫柔比星 |
英文名称 | Nemorubicin |
英文同义词 | Nemorubicin;5,12-Naphthacenedione, 7,8,9,10-tetrahydro-6,8,11-trihydroxy-8-(hydroxyacetyl)-1-methoxy-10-2,3,6-trideoxy-3-(2S)-2-methoxy-4-morpholinyl-.alpha.-L-lyxo-hexopyranosyloxy-, (8S,10S)-;methoxy-morpholynil-doxorubicin;NeMorubincine;(1S,3S)-3-Glycoloyl-1,2,3,4,6,11-hexahydro-3,5,12-trihydroxy-10-methoxy-6,11-dioxo-1-naphthacenyl 2,3,6-trideoxy-3-[(S)-2-methoxymorpholino]-alpha-L-lyxo-hexopyranoside;DMM Dox;FCE 23762;Methoxymorpholinyldoxorubicin |
CAS号 | 108852-90-0 |
分子式 | C32H37NO13 |
分子量 | 643.64 |
EINECS号 | |
相关类别 | 医药原料药;原料药【仅供科研】;科研原药系列;原料药;≧99% |
Mol文件 | 108852-90-0.mol |
结构式 |
奈莫柔比星 性质
沸点 | 852.2±65.0 °C(Predicted) |
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密度 | 1.55±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMSO:60.0(最大浓度 mg/mL);101.0(最大浓度 mM) |
酸度系数(pKa) | 7.35±0.60(Predicted) |
形态 | 粉末 |
Nemorubicin has antitumor activity, with IC
70
s of 578 nM, 468 nM, 193 nM, 191 nM, 68 nM, and 131 ± 9 nM for HT-29, A2780, DU145, EM-2, Jurkat and CEM cell lines, respectively.
Nemorubicin is CYP3A-activated anticancer prodrug, which can produce a more cytotoxic metabolite, PNU-159682.
Nemorubicin acts through nucleotide excision repair (NER) system to exert its activity. Nemorubicin (0-0.3 μM) is more active in the L1210/DDP cells with intact NER than in the XPG-deficient L1210/0 cells. Cells resistant to nemorubicin show increased sensitivity to UV damage.
Nemorubicin is cytotoxic to 9L/3A4 cells, with an IC
50
of 0.2 nM, 120-fold lower than that of P450-deficient 9L cells (IC
50
, 23.9 nM). Nemorubicin also potently inhibits Adeno-3A4 infected U251 cells with IC
50
of 1.4 nM. P450 reductase overexpression enhances cytotoxicity of Nemorubicin.
Nemorubicin is converted to PNU-159682 by human liver cytochrome P450 (CYP) 3A4 in rat, mouse, and dog liver microsomes. Nemorubicin (60 µg/kg) induces sifnificant tumor growth delay in scid mice bearing 9L/3A4 tumors, but shows no obvious effect on the tumor growth delay of 9L tumors in mice by i.v. or intratumoral injection (i.t.). Nemorubicin (40 µg/kg, i.p.) exhibits no antitumor activity and no host toxicity in mice bearing 9L/3A4 tumors.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/01/25 | HY-15794 | 奈莫柔比星 Nemorubicin | 108852-90-0 | 1mg | 600元 |
2024/01/25 | HY-15794 | 奈莫柔比星 Nemorubicin | 108852-90-0 | 5mg | 1500元 |