| 產品描述： | Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer |
| 靶點： |
ApoptosisCaspase;Bcl-2 Family;DNAAlkylation |
| 體外研究： |
Lobaplatin (D-19466, 0.25-32 μg/mL; 24-72 h) exhibits anti-proliferative activities against esophageal squamous cell carcinoma (ESCC) cell lines. Lobaplatin (0-16 μg/mL; 48 h) induces esophageal squamous cell carcinoma (ESCC) apoptosis and modulates expression of apoptosis-related proteins. Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) arrests cell cycle progression at G1 and G2/M phases in a time-dependent manner. Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) inhibits the mRNA levels of cyclin B, CDK1, and CDC25C phosphatase, down-regulates Rb/E2F complexes and up-regulates of CDK inhibitors. Cell Viability Assay Cell Line: KYSE-410 cells and EC-109 cells Concentration: 0.25, 0.5, 1, 2, 4, 8, 16 and 32 μg/mL Incubation Time: 24, 48 and 72 hours Result: Inhibited the growth of KYSE-410 and EC-109 cells in a dose- and time-dependent manner.Inhibited the clone formation activity of KYSE-410 and EC-109 cells in a dosedependent manner. Apoptosis Analysis Cell Line: KYSE-410 cells and EC-109 cells Concentration: 0.25, 1, 4 and 16 μg/mL Incubation Time: 48 hours Result: Increased the percentage of apoptotic cells in a dose-dependent manner. Western Blot Analysis Cell Line: KYSE-410 cells and EC-109 cells Concentration: 0, 1, 4 and 16 μg/mL Incubation Time: 48 hours Result: Increased expressions of cleaved-caspase-3, cleaved-caspase-8, cleaved-caspase-9 and Bax, while decreased expression of Bcl-2. Cell Cycle Analysis Cell Line: SMMC-7721 cells Concentration: 1.45 μg/mL Incubati |
| 體內研究： |
Lobaplatin (5 and 10 mg/kg; i.p.; once a week, for 3 weeks) suppresses tumor growth of esophageal squamous cell carcinoma (ESCC) xenograft. Animal Model: Male BALB/c nude mice (4-6 weeks) with ESCC xenograft Dosage: Intraperitoneal injection; once a week, for 3 weeks Administration: 5 and 10 mg/kg Result: Suppressed tumor volumes in a dose-dependent manner.Increased expressions of Bax and decreased expressions of Bcl-2. |
| 參考文獻： |
1. Du L, et, al. Antitumor activity of Lobaplatin against esophageal squamous cell carcinoma through caspase-dependent apoptosis and increasing the Bax/Bcl-2 ratio. Biomed Pharmacother. 2017 Nov;95:447-452. 2. Wu Q, et, al. Lobaplatin arrests cell cycle progression in human hepatocellular carcinoma cells. J Hematol Oncol. 2010 Oct 31;3:43. 3. McKeage MJ. Lobaplatin: a new antitumour platinum drug. Expert Opin Investig Drugs. 2001 Jan;10(1):119-28. |
| 溶解性： |
Soluble in H2O |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.517 ml |
12.584 ml |
25.169 ml |
| 5 mM |
0.503 ml |
2.517 ml |
5.034 ml |
| 10 mM |
0.252 ml |
1.258 ml |
2.517 ml |
| 50 mM |
0.05 ml |
0.252 ml |
0.503 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京