Cisplatin

Catalog No.S1166

Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells.

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Cisplatin Chemical Structure

Cisplatin Chemical Structure
Molecular Weight: 300.05

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Product Information

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Product Description

Biological Activity

Description Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells.
Targets DNA synthesis [1]
(Tumor cells)
In vitro Cisplatin induces cytotoxic by interaction with DNA to form DNA adducts which activate several signal transduction pathways, including Erk, p53, p73, and MAPK, which culminates in the activation of apoptosis. [1] Cisplatin (30 mM) treated for 6 h induces an apparent activation of Erk in HeLa cells, which is sustained over the following 14 h period. Cisplatin also shows an effective antineoplastic activity by inducing tumor cells death. Cisplatin displays ability to cause renal proximal tubular cell (RPTC) apoptosis, causing cell shrinkage, a 50-fold increase in caspase 3 activity, a 4-fold increase in phosphatidylserine externalization, and 5- and 15-fold increases in chromatin condensation and DNA hypoploidy, respectively. [4] Cisplatin (800 μM) causes typical features of necrosis of RPTC after treatment for 4 hr. [5]
In vivo Cisplatin has been demonstrated to be efficient in regression tumor growth in a wide variety of animal tumors models, including head and neck cancer xenografts, cervical squamous carcinoma xenografts, testicular carcinoma xenografts, ovarian cancer xenografts, breast carcinoma xenografts, colonic carcinoma, heterotransplanted hepatoblastoma, and so on. Cisplatin (5 mg/kg) given weekly i.v. at the day 1 and 7 induces a tumor growth inhibition (GI) of 77.5% and 85.1% of the serous xenografts Ov.Ri(C) and OVCAR-3, respectively. [6]
Features One of the most widely used and most potent chemotherapeutic agents.

Protocol(Only for Reference)

Cell Assay:

[3]

Cell lines Leukemia L1210/0 cells
Concentrations 7 μg/mL
Incubation Time 2 hours
Method

L1210/0 cells are maintained in an exponential suspension culture at 37 ℃ in a humidified atmosphere of 5% CO2 in McCoy's medium 5a (modified), supplemented with 15% calfserum, and Fungizone. L1210/0 cells are incubated in Cisplatin (7 μg/mL) for 2 hr at 37 ℃. To measure growth inhibition, the cells are centrifuged, washed once, resuspended in fresh medium at 30 × 103 to 50 × 103 cells/mL, and incubated for 3 days. Cell numbers are determined on a Coulter Counter. An aliquot of cells is diluted with an equal volume of 0.4% trypan blue. Viability is recorded as the percentage of cells that has excluded trypan blue. Cells incubated with Cisplatin as above are also diluted into 0.1% agar and allowed to grow for 2 weeks when colonies are counted.

Animal Study:

[6]

Animal Models The human ovarian cancer xenografts OVCAR-3 in nude mice
Formulation 0.9% NaCl solution
Dosages 5 mg/kg
Administration Given i.v. at day 0 (when tumors had reached a volume between 50 and 150 mm3) and day 7.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Siddik ZH. Oncogene, 2003, 22(47), 7265-7279.

[2] Wang X, et al. J Biol Chem, 2000, 275(50), 39435-39443.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02775812 Not yet recruiting Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage II  ...more Stage III Hypopharyngeal Squamous Cell Carcinoma|Stage III Laryngeal Squamous Cell Carcinoma|Stage III Oral Cavity Squamous Cell Carcinoma|Stage III Oropharyngeal Squamous Cell Carcinoma|Stage IVA Hypopharyngeal Squamous Cell Carcinoma|Stage IVA Laryngeal Squamous Cell Carcinoma|Stage IVA Oral Cavity Squamous Cell Carcinoma|Stage IVA Oropharyngeal Squamous Cell Carcinoma|Stage IVB Hypopharyngeal Squamous Cell Carcinoma|Stage IVB Laryngeal Squamous Cell Carcinoma|Stage IVB Oral Cavity Squamous Cell Carcinoma|Stage IVB Oropharyngeal Squamous Cell Carcinoma National Cancer Institute (NCI) December 2016 Phase 1
NCT02624999 Not yet recruiting Squamous Cell Carcinoma Head and Neck Immunovative Therapies, Ltd. December 2016 Phase 2
NCT01631357 Not yet recruiting Lung Cancer Tianjin Medical University Cancer Institute and Hospital November 2016 Phase 2|Phase 3
NCT02819999 Not yet recruiting Small Cell Lung Cancer Stemcentrx October 2016 Phase 1
NCT02724579 Not yet recruiting Untreated Childhood Medulloblastoma Childrens Oncology Group|National Cancer Institute (NCI) October 2016 Phase 2

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Chemical Information

Download Cisplatin SDF
Molecular Weight (MW) 300.05
Formula

Cl2H6N2Pt

CAS No. 15663-27-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMF 12 mg/mL (39.99 mM)
Water 0.01 mg/mL (0.03 mM)
Ethanol 0.01 mg/mL (0.03 mM)
In vivo Saline 3mg/mL
* The use of DMSO to dissolve platinum complex in biological studies is strongly discouraged. The DMSO inserts itself into the ligand.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Platinum, diamminedichloro-, (SP-4-2)-

Frequently Asked Questions

  • Question 1
    What is the appropriate concentration of DMF for cell culture and animal study?

    Answer: It depends on the cell type. The final concentration of DMF should be better limited to less than 0.1% if possible, or below 1%. Using saline as a vehicle for cisplatin at up to 3mg/ml is recommended. it's a suspension and can be administrated via oral gavage.

  • Question 2
    Your datasheet said that using DMF and DMSO as solvents to prepair stock solutions of cisplatin(Cat.No.S1166) is recommended. But using DMSO as the solvent would inactivate platinium complex as the paper reported?

    Answer: DMSO will inactivate platin-containing compounds. DMF is a much better choice than DMSO so you can dissolve cisplatin in DMF at up to 12mg/ml. It can also be dissolve in water at 0.01mg/ml.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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