Cisplatin
- 貨號 Cat. No.
- S1166
- 規格 Size
- 10mM/1mLã€50mg
- 品牌 Brand
- Selleckchem
Description
Cisplatin
Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts.
| Size | Price | Stock | Quantity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts. | |||||
|---|---|---|---|---|---|---|
| Targets | ||||||
| IC50 | ||||||
| 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:
| 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:
| Animal Models | The human ovarian cancer xenografts OVCAR-3 in nude mice |
|---|---|
| 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. |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01980667 | Not yet recruiting | Advanced Solid Tumors | PharmaMar | 2014-02 | Phase 1 |
| NCT01969578 | Not yet recruiting | Salivary Gland Cancer | European Organisation for Research and Treatment of Cancer - EORTC | 2014-03 | Phase 2 |
| NCT01451853 | Not yet recruiting | Lung Cancer|Head and Neck Cancer|Hearing Loss|Ototoxicity|Tinnitus|Neuropathy | Sound Pharmaceuticals, Incorporated|VA Puget Sound Health Care System | 2014-03 | Phase 2 |
| NCT01998529 | Not yet recruiting | Lung Cancer | M.D. Anderson Cancer Center | 2014-05 | Phase 1 |
| NCT01867086 | Not yet recruiting | Stage III Ovarian Cancer|Stage IV Ovarian Cancer | Gradalis, Inc. | 2014-06 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 300.05 |
|---|---|
| Formula | Cl2H6N2Pt |
| CAS No. | 15663-27-1 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | cisplatinum, CDDP, Platinol and Platinol-AQ |
| Solubility (25°C) * | In vitro | DMSO | 60 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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)- |
|---|
Customer Reviews (2)
![]() Click to enlarge | Rating | |
| Source | Dr. Edita Aksamitiene from Thomas Jefferson University.Cisplatin purchased from Selleck | |
| Method | Cell viability assay | |
| Cell Lines | pancreatic cancer cells | |
| Concentrations | 0-1000 nM | |
| Incubation Time | 72 h | |
| Results | Cisplatin potently inhibited the survival of Capan-2 cells in a dose-dependent manner. |
Product Citations (8)
SIRT1 and AMPK mediate hypoxia-induced resistance of non-small cell lung cancers to cisplatin and doxorubicin. [Shin DH, et al. Cancer Res 2013;74(1):298-308]
Targeting Sonic Hedgehog-Associated Medulloblastoma through Inhibition of Aurora and Polo-like Kinases. [Markant SL, et al. Cancer Res 2013;73(20):6310-22]
Phosphodiesterase 5 inhibitors enhance chemotherapy killing in gastrointestinal/genitourinary cancer cells. [Booth L , et al. Mol Pharmacol 2013;85(3):408-19]
