S89231 |
Lobaplatin |
源葉(MedMol) | 98% |
- 產(chǎn)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(diǎn): 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(nèi)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(xiàn):
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
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)