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Nedaplatin

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Chemical Structure| 95734-82-0 同义名 : 顺式-乙醇酸二氨合铂(II) ;NSC 375101D;NSC 375101
CAS号 : 95734-82-0
货号 : A101377
分子式 : C2H8N2O3Pt
纯度 : 99%+
分子量 : 303.175
MDL号 : MFCD00866374
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 8 mg/mL(26.39 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • DNA synthesis
描述 Nedaplatin is a derivative of cisplatin which produced less nausea & vomiting and nephrotoxicity. In the phase I study, the MTD was 120 mg/m2 and the DLF was a bone marrow suppression[3]. he topoisomerase I-inhibitory effect of 7-ethyl-1-hydroxy-CPT was enhanced 10-fold in the presence of Nedaplatin (NSC 375101D, NDP) at microgram/milliliter concentrations[4]. Nedaplatin (NSC 375101D, NDP) was developed as a second generation platinum complex. Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP). At the high-dose of Nedaplatin (NSC 375101D, NDP) in FN therapy, a reduction of tumour size and long-term tumour-free survival were frequently observed. The survival effect of the combinations of Nedaplatin (NSC 375101D, NDP) with 5-FU was superior to those of the combination of CDDP with 5-FU. In conclusion, the sequence-dependent antitumour efficacy and toxicity of the combination of NDP or CDDP with 5-FU was demonstrated in this study, and FN therapy appeared to be the most efficient regimen as a clinical therapy[5]. Autophagy played a cytoprotective role in nedaplatin-induced cytotoxicity of HNE1/DDP and CNE2/DDP cells[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
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 <<
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 <<
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

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.49mL

3.30mL

1.65mL

32.98mL

6.60mL

3.30mL
参考文献

[1]Wheate NJ, Walker S, Craig GE, Oun R. The status of platinum anticancer drugs in the clinic and in clinical trials. Dalton Trans. 2010 Sep 21;39(35):8113-27.

[2]Alberts DS, Fanta PT, et al. In vitro phase II comparison of the cytotoxicity of a novel platinum analog, nedaplatin (254-S), with that of cisplatin and carboplatin against fresh, human ovarian cancers. Cancer Chemother Pharmacol. 1997;39(6):493-7.

[3]Ota K. [Nedaplatin]. Gan To Kagaku Ryoho. 1996 Feb;23(3):379-87. Japanese

[4]Kanzawa F, Koizumi F, Koh Y, Nakamura T, Tatsumi Y, Fukumoto H, Saijo N, Yoshioka T, Nishio K. In vitro synergistic interactions between the cisplatin analogue nedaplatin and the DNA topoisomerase I inhibitor irinotecan and the mechanism of this interaction. Clin Cancer Res. 2001 Jan;7(1):202-9

[5]Uchida N, Takeda Y, Hojo K, Maekawa R, Sugita K, Yoshioka T. Sequence-dependent antitumour efficacy of combination chemotherapy of nedaplatin, a novel platinum complex, with 5-fluorouracil in an in vivo murine tumour model. Eur J Cancer. 1998 Oct;34(11):1796-801

[6]Liu Z, Liu J, Li L, Nie D, Tao Q, Wu J, Fan J, Lin C, Zhao S, Ju D. Inhibition of Autophagy Potentiated the Antitumor Effect of Nedaplatin in Cisplatin-Resistant Nasopharyngeal Carcinoma Cells. PLoS One. 2015 Aug 19;10(8):e0135236