产品说明书
Lobaplatin
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同义名 : | D-19466 |
| CAS号 : | 135558-11-1 | |
| 货号 : | A657863 | |
| 分子式 : | C9H18N2O3Pt | |
| 纯度 : | 98+% | |
| 分子量 : | 397.329 | |
| MDL号 : | MFCD00866545 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 50 mg/mL(125.84 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links. Lobaplatin influences the expression of the c-myc gene, which is involved in oncogenesis, apoptosis and cell proliferation[3]. Lobaplatin and paclitaxel inhibited SGC-7901 cell growth in a concentration and timedependent manner, with IC25 values at 48h of 1.97±0.17µg/ml and 1.98±0.19 ng/ml, respectively. Lobaplatin did not affect cyclin D1 and CDK4 protein expression, while cyclin E1 and CDK2 levels were significantly increased, with cyclin B1 amounts markedly decreased (p<0.05). More S phase cells were observed after lobaplatin treatment compared with controls (60.03±1.25 vs. 18.69±0.96%; p<0.05). Lobaplatin and paclitaxel combination did not affect cyclin D1 and CDK4 protein levels (p>0.05); meanwhile, cyclin E1 and CDK2 levels were increased, with reduced cyclin B1 amounts, compared with control values (p<0.05)[4].Lobaplatin inhibited proliferation of human HCC cells in a dose-dependent manner. For the most sensitive SMMC-7721 cells, lobaplatin arrested cell cycle progression in G1 and G2/M phases time-dependently which might be associated with the down-regulation of cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and the up-regulation of p53, p21, and p27[5].Lobaplatin inhibited the proliferation of human gastric cancer cells and induced apoptosis, which may be associated with the up-regulation of Bax expression, poly(ADP-ribose) polymerase (PARP) cleavage, p53 expression and the reduction of Bcl-2 expression[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03731442 | Esophageal Cancer | Phase 3 | Recruiting | October 31, 2027 | China, Beijing ... 展开 >> Department of Radiation Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD 收起 << |
| NCT03328234 | IMRT With or Without Concurren... 展开 >>t Chemotherapy for Esophageal Cancer 收起 << | Phase 3 | Recruiting | December 31, 2022 | China ... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, China, 100021 Contact: Xin Wang, MD +861013311583220 beryl_wx2000@163.com 收起 << |
| NCT03308552 | Esophageal Neoplasms | Phase 3 | Recruiting | August 30, 2021 | China, Beijing ... 展开 >> Department of Radiation Oncology, Cancer Hospital, National Cancer Center, Chinese Academy of Medical Sciences (CAMS) and Peking Union Medical College (PUMC) Recruiting Beijing, Beijing, China, 100021 Contact: Zefen Xiao, MD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.58mL 2.52mL 1.26mL |
25.17mL 5.03mL 2.52mL |
| 参考文献 |
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