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Cisplatin

Catalog No. T1564 CAS 15663-27-1

Synonyms: cis-Diaminodichloroplatinum, CDDP

Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates iron death and induces autophagy.

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Cisplatin, CAS 15663-27-1

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50 mg	In stock	$ 28.00
100 mg	In stock	$ 42.00
500 mg	In stock	$ 97.00

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Purity: 99.62%

Purity: 99.6%

Purity: 99.54%

Purity: 99.27%

Purity: 98.11%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates iron death and induces autophagy.
In vitro	METHODS: Human non-small cell lung cancer cells A549, SKMES-1, MOR and H460 were treated with Cisplatin (0.001-100 μM) for 72 h, and cell growth inhibition was detected by MTT. RESULTS: Cisplatin dose-dependently inhibited the cell growth of A549, SKMES-1, MOR and H460 cells with IC50 of 1.58 µM, 4.09 µM, 6.39 µM and 5.72 µM, respectively. [1] METHODS: Human breast cancer MCF-7 and MDA-MB-231 were treated with Cisplatin (2-10 μg/mL) for 48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Cisplatin dose-dependently induced increased levels of apoptosis-related proteins cleaved-caspase 3 and cleaved-PARP in MCF-7 and MDA-MB-231 cells. [2] METHODS: Mesothelioma cells JU77, LO68 and ONE58 were treated with Cisplatin (5-100 μg/mL) for 24 h, and mitochondrial membrane potential (MMP) was detected using JC-1 dye. RESULTS: Cisplatin dose-dependently decreased MMP and inhibited mitochondrial function in JU77, LO68 and ONE58 cells. [3]
In vivo	METHODS: To assay anti-tumor activity in vivo, Cisplatin (5 mg/kg/6 days) and Chloroquine (13 mg/kg/day) were intraperitoneally injected into BALB/c nude mice bearing hypopharyngeal squamous cell carcinoma tumors (HSCC) FaDu for eighteen days. RESULTS: Cisplatin treatment significantly inhibited HSCC tumor growth. Chloroquine inhibited autophagy and increased Cisplatin-induced apoptosis, which enhanced the efficacy of Cisplatin, resulting in reduced tumor growth and prolonged survival in mice. [4] METHODS: To attenuate nephrotoxicity induced by Cisplatin treatment, Cisplatin (3-6 mg/kg/3 days) was administered intraperitoneally and Cilastatin (100 mg/kg/day) subcutaneously to BALB/c mice with human lung adenocarcinoma tumor A549 for seven days. RESULTS: Cilastatin can reduce the induced nephrotoxicity of Cisplatin without affecting its antitumor effects. [5]
Cell Research	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].
Animal Research	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].

Synonyms	cis-Diaminodichloroplatinum, CDDP
Molecular Weight	300.04
Formula	Cl2H6N2Pt
CAS No.	15663-27-1

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 3.33mg/ml(11.1mM), Sonification is recommended. (DMSO inactivates the activity of Cisplatin.The compound is unstable in solution, please use soon.)

DMF: 20mg/ml(66.7mM)

References and Literature

1. Barr MP, et al. Generation and characterisation of cisplatin-resistant non-small cell lung cancer cell lines displaying a stem-like signature. PLoS One. 2013;8(1):e54193. 2. Jiang Y, et al. Cisplatin-induced autophagy protects breast cancer cells from apoptosis by regulating yes-associated protein. Oncol Rep. 2017 Dec;38(6):3668-3676. 3. Cregan IL, et al. Mechanisms of cisplatin-induced cell death in malignant mesothelioma cells: role of inhibitor of apoptosis proteins (IAPs) and caspases. Int J Oncol. 2013 Feb;42(2):444-52. 4. Zhao XG, et al. Chloroquine-enhanced efficacy of cisplatin in the treatment of hypopharyngeal carcinoma in xenograft mice. PLoS One. 2015 Apr 29;10(4):e0126147. 5. Arita M, et al. Combination therapy of cisplatin with cilastatin enables an increased dose of cisplatin, enhancing its antitumor effect by suppression of nephrotoxicity. Sci Rep. 2021 Jan 12;11(1):750. 6. Shao C S, Zhou X H, Zheng X X, et al. Ganoderic acid D induces synergistic autophagic cell death except for apoptosis in ESCC cells[J]. Journal of Ethnopharmacology. 2020, 262: 113213. 7. Wu Y, Zhou L, Wang Z, et al. Systematic screening for potential therapeutic targets in osteosarcoma through a kinome-wide CRISPR-Cas9 library[J]. Cancer Biology & Medicine. 2020, 17(3): 782. 8. Wang C, Xiong M, Yang C, et al. PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury[J]. Journal of Medicinal Chemistry. 2020 9. Kang C L, Qi B, Cai Q Q, et al. LncRNA AY promotes hepatocellular carcinoma metastasis by stimulating ITGAV transcription. Theranostics. 2019, 9(15): 4421. 10. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma[J]. Cancer Research.

Citations

1. Zhu C, Xie Y, Li Q, et al.CPSF6-mediated XBP1 3’UTR shortening attenuates cisplatin-induced ER stress and elevates chemo-resistance in lung adenocarcinoma.Drug Resistance Updates.2023: 100933. 2. Yang C, Xu H, Yang D, et al.A renal YY1-KIM1-DR5 axis regulates the progression of acute kidney injury.Nature Communications.2023, 14(1): 4261. 3. Liu X, Cen X, Wu R, et al.ARIH1 activates STING-mediated T-cell activation and sensitizes tumors to immune checkpoint blockade.Nature Communications.2023, 14(1): 4066. 4. Bi G, Liang J, Shan G, et al.Retinol saturase mediates retinoid metabolism to impair a ferroptosis defense system in cancer cells.Cancer Research.2023: CAN-22-3977. 5. Zhao X, Lian X, Xie J, et al.Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment.Redox Biology.2023: 102678. 6. Qu Y Q, Song L L, Xu S W, et al.Pomiferin targets SERCA, mTOR, and P-gp to induce autophagic cell death in apoptosis-resistant cancer cells, and reverses the MDR phenotype in cisplatin-resistant tumors in vivo.Pharmacological Research.2023: 106769. 7. Yang D, Fan Y, Xiong M, et al.Loss of renal tubular G9a benefits acute kidney injury by lowering focal lipid accumulation via CES1.EMBO reports.2023: e56128. 8. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567. 9. Zhao G, Liang J, Shan G, et al.KLF11 regulates lung adenocarcinoma ferroptosis and chemosensitivity by suppressing GPX4.Communications Biology.2023, 6(1): 570. 10. Song M, Fang Z, Wang J, et al.A Nano-targeted Co-delivery System Based on Gene Regulation and Molecular Blocking Strategy for Synergistic Enhancement of Platinum Chemotherapy Sensitivity in Ovarian Cancer.International Journal of Pharmaceutics.2023: 123022.

11. Ma X Y, Xu H Q, Zhao J F, et al.Discovery of a Novel Bloom’s Syndrome Protein (BLM) Inhibitor Suppressing Growth and Metastasis of Prostate Cancer.International journal of molecular sciences.2022, 23(23): 14798. 12. Lin X, Chen J, Li X, et al.Dimeric oxyberberine CT4-1 targets LINC02331 to induce cytotoxicity and inhibit chemoresistance via suppressing Wnt/β-catenin signaling in hepatocellular carcinoma.Archives of Toxicology.2023: 1-21. 13. Wu Z, Yuan C, Zhang Z, et al.Paris saponins Ⅶ inhibits glycolysis of ovarian cancer via the RORC/ACK1 signaling pathway.Biochemical Pharmacology.2023: 115597. 14. Ma X Y, Zhao J F, Ruan Y, et al.ML216-Induced BLM Helicase Inhibition Sensitizes PCa Cells to the DNA-Crosslinking Agent Cisplatin.Molecules.2022, 27(24): 8790. 15. Bu X, Zhang J, Sun H, et al.SEC61 translocon subunit gamma enhances low-dose cisplatin-induced cancer-stem cell properties of head and neck squamous cell carcinoma via enhancing Ca2+-mediated autophagy.Journal of Dental Sciences.2023 16. Liang J, Zhao G, Bian Y, et al.HNF4G increases cisplatin resistance in lung adenocarcinoma via the MAPK6/Akt pathway.PeerJ.2023, 11: e14996. 17. Li J, Kou Y, Zhang X, et al.Biochanin A inhibits lung adenocarcinoma progression by targeting ZEB1.Discover Oncology.2022, 13(1): 1-14. 18. Wu L L, Jiang W M, Liu Z Y, et al.AMG-510 and cisplatin combination increases antitumor effect in lung adenocarcinoma with mutation of KRAS G12C: a preclinical and translational research.Discover Oncology.2023, 14(1): 91. 19. Chen Y, Shi J, Wang X, et al.An antioxidant feedforward cycle coordinated by linker histone variant H1. 2 and NRF2 that drives nonsmall cell lung cancer progression.Proceedings of the National Academy of Sciences.2023, 120(39): e2306288120. 20. Pak M E, Park Y J, Yang H J, et al. Samhwangsasim-tang attenuates neuronal apoptosis and cognitive decline through BDNF-mediated activation of tyrosin kinase B and p75-neurotrophin receptors. Phytomedicine. 2022: 153997. 21. Wang P, Yang W, Guo H, et al. IL‐36γ and IL‐36Ra Reciprocally Regulate NSCLC Progression by Modulating GSH Homeostasis and Oxidative Stress‐Induced Cell Death. Advanced Science. 2021: 2101501. 22. Glorieux C, Xia X, You X, et al. Cisplatin and gemcitabine exert opposite effects on immunotherapy with PD-1 antibody in K-ras-driven cancer. Journal of Advanced Research. 2021 23. Zhang T, Xu C, Zheng P, et al. Glaucocalyxin B Attenuates Ovarian Cancer Cell Growth and Cisplatin Resistance In Vitro via Activating Oxidative Stress. Oxidative Medicine and Cellular Longevity. 2022 24. Feng J, Xi Z, Jiang X, et al. Saikosaponin a enhances Docetaxel efficacy by selectively inducing death of dormant prostate cancer cells through excessive autophagy. Cancer Letters. 2022: 216011. 25. Liu L, Liu S, Deng P, et al. Targeting the IRAK1-S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021 Mar 1;81(5):1413-1425. doi: 10.1158/0008-5472.CAN-20-2125. Epub 2021 Jan 5. 26. Liu L, Liu S, Deng P, et al. Targeting the IRAK1–S100A9 Axis Overcomes Resistance to Paclitaxel in Nasopharyngeal Carcinoma. Cancer Research. 2021, 81(5): 1413-1425. 27. Bi G, Liang J, Zhao M, et al. MiR-6077 promotes cisplatin/pemetrexed resistance in lung adenocarcinoma by targeting CDKN1A/cell cycle arrest and KEAP1/ferroptosis pathways. Molecular Therapy-Nucleic Acids. 2022 28. Kang C L, Qi B, Cai Q Q, et al. LncRNA AY promotes hepatocellular carcinoma metastasis by stimulating ITGAV transcription. Theranostics. 2019, 9(15): 4421 29. Luo X, Cai G, Guo Y, et al. Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry.. 30. Lü Z, Li X, Li K, et al. Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes. Biochemical Pharmacology. 2022: 114913. 31. Wang C, Xiong M, Yang C, et al. PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury. Journal of Medicinal Chemistry. 2020 32. Wu Y, Zhou L, Wang Z, et al. Systematic screening for potential therapeutic targets in osteosarcoma through a kinome-wide CRISPR-Cas9 library. Cancer Biology & Medicine. 2020, 17(3): 782. 33. Cheng Y, Wang Q, Zhang Z, et al. Saucerneol attenuates nasopharyngeal carcinoma cells proliferation and metastasis through selectively targeting Grp94. Phytomedicine. 2022: 154133 34. Zhang H, Shan G, Jin X, et al. ARNTL2 is an indicator of poor prognosis, promotes epithelial-to-mesenchymal transition and inhibits ferroptosis in lung adenocarcinoma. Translational Oncology. 2022, 26: 101562. 35. Shao C S, Zhou X H, Zheng X X, et al. Ganoderic acid D induces synergistic autophagic cell death except for apoptosis in ESCC cells. Journal of Ethnopharmacology. 2020, 262: 113213. 36. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization. Reproduction. 2021, 1(aop). 37. Kong F, Liu X, Zhou Y, et al. Downregulation of METTL14 increases apoptosis and autophagy induced by cisplatin in pancreatic cancer cells. The International Journal of Biochemistry & Cell Biology. 2020: 105731 38. Guo X, Fang Z, Zhang M, et al. A Co-Delivery System of Curcumin and p53 for Enhancing the Sensitivity of Drug-Resistant Ovarian Cancer Cells to Cisplatin. Molecules. 2020, 25(11): 2621 39. Kasiram M Z, Hapidin H, Abdullah H, et al. Tannic acid enhances cisplatin effect on cell proliferation and apoptosis of human osteosarcoma cell line (U2OS). Pharmacological Reports. 2021: 1-14. 40. Sun J, Liu W, Li Y, et al. An on-chip cell culturing and combinatorial drug screening system. Microfluidics and Nanofluidics. 2017 Jul 21(7): 125. 41. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 42. Su W, Li Y, Zhang L, et al. Typography-Like 3D-Printed Templates for the Lithography-Free Fabrication of Microfluidic Chips. SLAS TECHNOLOGY: Translating Life Sciences Innovation. 2019: 2472630319867903. 43. Liu S, Chai T, Garcia-Marques F, et al.UCHL1 is a potential molecular indicator and therapeutic target for neuroendocrine carcinomas.Cell Reports Medicine.2024 44. Zhang H, Li Q, Guo X, et al.MGMT activated by Wnt pathway promotes cisplatin tolerance through inducing slow-cycling cells and nonhomologous end joining in colorectal cancer.Journal of Pharmaceutical Analysis.2024 45. Tan X D, Luo C F, Liang S Y.Antihyperlipidemic drug rosuvastatin suppressed tumor progression and potentiated chemosensitivity by downregulating CCNA2 in lung adenocarcinoma.Journal of Chemotherapy.2024: 1-13. 46. Liu Y, Wu Q, Jiang B, et al.Distinct regulation of ASCL1 by the cell cycle and chemotherapy in small cell lung cancer.Molecular Cancer Research.2024 47. Bi G, Liang J, Bian Y, et al.Polyamine-mediated ferroptosis amplification acts as a targetable vulnerability in cancer.Nature Communications.2024, 15(1): 2461. 48. Li Y, Li G, Zuo C, et al.Discovery of ganoderic acid A (GAA) PROTACs as MDM2 protein degraders for the treatment of breast cancer.European Journal of Medicinal Chemistry.2024, 270: 116367.

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This product is contained In the following compound libraries：

Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Anti-Liver Cancer Compound Library Anti-Lung Cancer Compound Library Human Metabolite Library

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Keywords

Cisplatin 15663-27-1 Apoptosis Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA Alkylator/Crosslinker Ferroptosis DNA/RNA Synthesis cis-Platinum drug cross-linking cis-Diaminodichloroplatinum antineoplastic damage CDDP inhibit Inhibitor chemotherapy DNA inhibitor

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