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9-硝基喜树碱

9-硝基喜树碱用途

Rubitecan (RFS 2000),喜树碱衍生物,是一种口服活性拓扑异构酶 I 抑制剂,具有广泛抗肿瘤活性,诱导蛋白质连接的 DNA 单链断裂,从而阻断分裂细胞中的 DNA 和 RNA 合成。

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9-硝基喜树碱名称

[ CAS 号 ]:
91421-42-0

[ 中文名 ]:
鲁比替康

[ 英文名 ]:
rubitecan

[中文别名 ]:

[英文别名 ]:

rubitecan
MFCD06656294
PYRIDOXINE 3,4-DIPALMITATE
9-nitro-20(s)-camptothecin
Orathecin

9-硝基喜树碱生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

[ 靶点 ]

Topoisomerase I[1]

[体外研究]

Rubitecan(RFS 2000)分别用IC50S 0.32、0.83和7.7μm抑制U-CH1、U-CH2和CCL4细胞[4]。

[参考文献]

[1]. Burris HA 3rd, et al. Phase II trial of oral rubitecan in previously treated pancreatic cancer patients. Oncologist. 2005 Mar;10(3):183-90.

[2]. Rubitecan: 9-NC, 9-Nitro-20(S)-camptothecin, 9-nitro-camptothecin, 9-nitrocamptothecin, RFS 2000, RFS2000. Drugs R D. 2004;5(5):305-11.

[3]. Rubitecan

[4]. Xia M, et al. Identification of repurposed small molecule drugs for chordoma therapy. Cancer Biol Ther. 2013 Jul;14(7):638-47.

9-硝基喜树碱物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
816.3±65.0 °C at 760 mmHg

[ 熔点 ]:
182-186ºC

[ 分子式 ]:
C₂₀H₁₅N₃O₆

[ 分子量 ]:
393.350

[ 闪点 ]:
447.5±34.3 °C

[ 精确质量 ]:
393.096100

[ PSA ]:
127.24000

[ LogP ]:
1.38

[ 外观性状 ]:
黄色非晶形的粉末

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.762

[ 储存条件 ]:
Room temp

9-硝基喜树碱MSDS

9-硝基喜树碱安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UQ0493300

9-硝基喜树碱合成路线

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9-硝基喜树碱文献

Effect of injection routes on pharmacokinetics and lactone/carboxylate equilibrium of 9-Nitrocamptothecin in rats.

Int. J. Pharm. 340(1-2) , 29-33, (2007)

Pharmacokinetics and lactone/carboxylate equilibrium of 9-Nitrocamptothecin (9-NC) were compared after intravenous (i.v.) and intramuscular (i.m.) injection at a dose of 1.5mg/kg 9-NC solution. The co...

Effect of phospholipid composition on characterization of liposomes containing 9-nitrocamptothecin.

Drug Dev. Ind. Pharm. 32(6) , 719-26, (2006)

9-Nitrocamptothecin (9-NC), a newly developed camptothecin derivative, had poor solubility in any pharmaceutically acceptable solvents. One way of improving the solubility is to formulate the drug int...

Sequential oral 9-nitrocamptothecin and etoposide: a pharmacodynamic- and pharmacokinetic-based phase I trial.

Mol. Cancer Ther. 5(8) , 2130-7, (2006)

Resistance to topoisomerase (topo) I inhibitors has been related to down-regulation of nuclear target enzyme, whereas sensitization to topo II inhibitors may result from induction of topo II by topo I...

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