| 名稱 | Cisplatin |
| 描述 | Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure. |
| 細胞實驗 | Rabbit renal proximal tubules were isolated using the iron oxide perfusion method and grown in 35-mm tissue culture dishes under improved conditions as described previously. The cell culture medium was a 1:1 mixture of Dulbecco's modified Eagle's medium/Ham's F-12 (without D-glucose, phenol red, or sodium pyruvate) supplemented with 15 mM HEPES buffer, 2.5 mM L-glutamine, 1 μM pyridoxine HCl, 15 mM sodium bicarbonate, and 6 mM lactate. Hydrocortisone (50 nM), selenium (5 ng/ml), human transferrin (5 μg/ml), bovine insulin (10 nM), and L-ascorbic acid-2-phosphate (50 μM) were added to fresh culture medium immediately before daily media change. In general, confluent RPTCs were treated with inhibitors or diluent control [typically DMSO at 0.1% (v/v)] for 30 min before treatment with cisplatin. Aliquots of RPTCs were used for various assays as detailed below [1]. |
| 動物實驗 | Mice were divided randomly into three groups (Control, Cisplatin and Cisplatin+HemoHIM), and each group consisted of twenty mice. B16F0 melanoma (5 × 10^5 cells/mouse) was inoculated into subcutaneous femoral left region of mice at 3 days before an initial injection of cisplatin. Cisplatin was injected intraperitoneally at 4 mg/kg body weight (B.W.) on day 0, 7 and 14 (total three injections). Experimental group was intubated with HemoHIM at a final concentration of 100 mg/kgB.W. by everyday from day -1 to day 16, while the control group received only water. On day 17 after initial injection of cisplatin, all mice of each group were experimented, respectively, to evaluate tumor weight or tumor size. The tumor size was calculated as follows: tumor size = ab^2/2, where a and b are the larger and smaller diameters, respectively [3]. |
| 體外活性 | 方法：人非小細胞肺癌細胞 A549、SKMES-1、MOR 和 H460 用 Cisplatin (0.001-100 μM) 處理 72 h，使用 MTT 方法檢測細胞生長抑制情況。
結果：Cisplatin 劑量依賴性地抑制 A549、SKMES-1、MOR 和 H460 細胞生長，IC50 分別為 1.58 μM、4.09 μM、6.39 μM 和 5.72 μM。[1]
方法：人乳腺癌 MCF-7 和 MDA-MB-231 用 Cisplatin (2-10 μg/mL) 處理 48 h，使用 Western Blot 方法檢測靶點蛋白表達水平。
結果：Cisplatin 劑量依賴性誘導 MCF-7 和 MDA-MB-231 細胞中凋亡相關蛋白 cleaved-caspase 3 和 cleaved-PARP 的水平增加。[2]
方法：間皮瘤細胞 JU77、LO68 和 ONE58 用 Cisplatin (5-100 μg/mL) 處理 24 h，使用 JC-1 染料檢測線粒體膜電位 (MMP)。
結果：Cisplatin 劑量依賴性降低 JU77、LO68 和 ONE58 細胞的 MMP，抑制線粒體功能。[3] |
| 體內(nèi)活性 | 方法：為檢測體內(nèi)抗腫瘤活性，將 Cisplatin (5 mg/kg/6 天) 和 Chloroquine (13? mg/kg/天) 腹腔注射給攜帶咽下鱗狀細胞癌腫瘤 (HSCC) FaDu 的 BALB/c nude 小鼠，持續(xù)十八天。
結果：Cisplatin 治療顯著抑制 HSCC 腫瘤生長，Chloroquine 抑制自噬并增加 Cisplatin 誘導的細胞凋亡，從而增強了 Cisplatin 的療效，導致小鼠的腫瘤生長減少和生存期延長。[4]
方法：為減輕 Cisplatin 治療引起的腎毒性，將 Cisplatin (3-6 mg/kg/3天) 腹腔注射和 Cilastatin (100? mg/kg/天) 皮下注射給人肺腺癌腫瘤 A549 的 BALB/c 小鼠，持續(xù)七天。
結果：Cilastatin 可以在不影響 Cisplatin 抗腫瘤作用的情況下減少其誘導的腎毒性。[5] |
| 存儲條件 | Keep away from direct sunlight,The compound is unstable in solution. Please use soon
Powder: -20°C for 3 years
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : 1 mg/mL (3.3 mM), Heating to 50℃ is recommended. The compound is unstable in solution. Please use soon.（DMSO can inactivate Cisplatin's activity.)
DMSO : Soluble, DMSO inactivates the activity of Cisplatin.
DMF : 20 mg/mL (66.66 mM), Sonication is recommended. The compound is unstable in solution. Please use soon.
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| 關鍵字 | RNASynthesis | RNA Synthesis | Inhibitor | inhibit | Ferroptosis | drug | DNASynthesis | DNAAlkylator | DNA synthesis | DNA Alkylator/Crosslinker | DNA Alkylator | DNA | damage | cross-linking | Crosslinker | cis-Platinum | Cisplatin | chemotherapy | Autophagy | antineoplastic |
| 相關產(chǎn)品 | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Hemin | Hydroxychloroquine | Sildenafil citrate | Stavudine | Tamoxifen | Thymidine | Paeonol |