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首页 / 抑制剂/激动剂 / DNA损伤 / DNA烷基化剂/交联剂 / Nedaplatin

Nedaplatin {[allProObj[0].p_purity_real_show]}

货号：A101377 同义名： 顺式-乙醇酸二氨合铂(II) / NSC 375101D; NSC 375101

Nedaplatin 是一种顺铂衍生物，对肿瘤克隆形成单位的 IC50 为 94 μM。

Nedaplatin 化学结构 CAS号：95734-82-0
Nedaplatin 化学结构
CAS号：95734-82-0
Nedaplatin 3D分子结构
CAS号：95734-82-0
Nedaplatin 化学结构 CAS号：95734-82-0
Nedaplatin 3D分子结构 CAS号：95734-82-0
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Nedaplatin 纯度/质量文件 产品仅供科研

货号：A101377 标准纯度： {[allProObj[0].p_purity_real_show]}
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Nedaplatin 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].

Nedaplatin 细胞实验

Cell Line
Concentration Treated Time Description References
HEK293 0.5, 1, 2, 4, 8, 10, 20 μg/mL 72 hours Evaluate the cytotoxicity of free and liposomal Nedaplatin on HEK293 cells. Results showed no significant increase in cytotoxicity with liposomal Nedaplatin. Pharmaceutics. 2020 Sep 10;12(9):863.
WI-38 0.5, 1, 2, 4, 8, 10, 20 μg/mL 72 hours Evaluate the cytotoxicity of free and liposomal Nedaplatin on WI-38 cells. Results showed no significant increase in cytotoxicity with liposomal Nedaplatin. Pharmaceutics. 2020 Sep 10;12(9):863.
U2OS 0.5, 1, 2, 4, 8, 10, 20 μg/mL 72 hours Evaluate the cytotoxicity of free and liposomal Nedaplatin on U2OS cells. Results showed that liposomal Nedaplatin significantly reduced cell viability at lower concentrations. Pharmaceutics. 2020 Sep 10;12(9):863.
A549 0.5, 1, 2, 4, 8, 10, 20 μg/mL 72 hours Evaluate the cytotoxicity of free and liposomal Nedaplatin on A549 cells. Results showed that liposomal Nedaplatin significantly increased cytotoxicity at all tested concentrations. Pharmaceutics. 2020 Sep 10;12(9):863.
MDA-MB-468 0.067 µM 24 hours Evaluate the cytotoxicity of nedaplatin on TNBC cells, results showed cytotoxicity to MDA-MB-468 cells at the highest tested dose Cell Death Discov. 2024 Jan 29;10(1):57.
BT-549 0.15 µM 24 hours Evaluate the cytotoxicity of nedaplatin on TNBC cells, results showed high cytotoxicity to CAL-148 cells at the highest tested dose Cell Death Discov. 2024 Jan 29;10(1):57.

Nedaplatin 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish HCC1806 and MCF-7 cell xenograft models 25 µM 48 hours Evaluate the effect of nedaplatin combined with bortezomib on tumor regression, results showed reduced tumor volume Cell Death Discov. 2024 Jan 29;10(1):57.

Nedaplatin 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 <<

Nedaplatin 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

Nedaplatin 实验方案

计算器
存储液制备 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

Nedaplatin 技术信息

CAS号95734-82-0
分子式C2H8N2O3Pt
分子量 303.17
SMILES Code O=C1[O-][Pt+2]([NH3])([NH3])[O-]C1
MDL No. MFCD00866374
别名 顺式-乙醇酸二氨合铂(II) ;NSC 375101D; NSC 375101
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

H2O: 8 mg/mL(26.39 mM)，配合低频超声，并水浴加热至45℃助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Nedaplatin | 95734-82-0 | NSC 375101D | DNA/RNA Synthesis | DNA/RNA Synthesis Inhibitor | Cell Cycle/DNA Damage | DNA/RNA Synthesis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Nedaplatin 纯度/质量文件 | Nedaplatin 生物活性 | Nedaplatin 临床数据 | Nedaplatin 参考文献 | Nedaplatin 实验方案 | Nedaplatin 技术信息

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