Cisplatin

CatalogusnummerS1166 Batch:S116618

Afdrukken

Technische gegevens

Formule

Cl2H6N2Pt
Moleculair gewicht 300.05 CAS-nr. 15663-27-1
Oplosbaarheid (25°C)* In vitro DMF 15 mg/mL (49.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Clear solution
5%DMF 40%PEG300 5%Tween80 50%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 0.750mg/ml (2.50mM) Taking the 1 mL working solution as an example, add 50 μL 15 mg/ml clarified DMF stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving Cisplatin is een anorganisch platina complex, dat in staat is om de DNA-synthese te remmen door DNA-adducten te vormen in tumorcellen. Cisplatin activeert ferroptosis en induceert autophagy.Oplossingen zijn instabiel en moeten vers worden bereid. DMSO wordt niet aanbevolen om platina-houdende medicijnen in op te lossen, wat gemakkelijk kan leiden tot inactivatie van het medicijn.
Doelen
DNA synthesis
(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.

This compound (30 μM) treated for 6 h induces an apparent activation of Erk in HeLa cells, which is sustained over the following 14 h period. It also shows an effective antineoplastic activity by inducing tumor cells death.

It 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.

This chemical (800 μM) causes typical features of necrosis of RPTC after treatment for 4 hr.

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. This compound (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.

Kenmerken Een van de meest gebruikte en krachtigste chemotherapeutische middelen. Dit product wordt niet aanbevolen om op te lossen in dimethylsulfoxide (DMSO).

Protocol (uit referentie)

Celassay:

[3]
  • Cellijnen

    Leukemia L1210/0 cells

  • Concentraties

    7 μg/mL

  • Incubatietijd

    2 hours

  • Methode

    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 this compound as above are also diluted into 0.1% agar and allowed to grow for 2 weeks when colonies are counted.
Dierstudie:

[7]
  • Dierlijke modellen

    Female NMRI/Cpb (nuinu) mice

  • Doseringen

    5 mg/kg

  • Toediening

    i.v.

Referenties

  • https://pubmed.ncbi.nlm.nih.gov/14576837/
  • https://pubmed.ncbi.nlm.nih.gov/10993883/
  • https://pubmed.ncbi.nlm.nih.gov/3395999/
  • https://pubmed.ncbi.nlm.nih.gov/12065694/
  • https://pubmed.ncbi.nlm.nih.gov/8967349/
  • https://pubmed.ncbi.nlm.nih.gov/1563830/
  • https://pubmed.ncbi.nlm.nih.gov/24812268/
  • https://pubmed.ncbi.nlm.nih.gov/28494534/

Klantproductvalidatie

<p>Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05.</p>

Gegevens van [ Cancer Res , 2014 , 74(1), 298-308 ]

Gegevens van [ PLoS One , 2013 , 8(1), e54595 ]

<p> </p><p>Growth inhibitory effects of Cisplatin human pancreatic cancer cells. Capan-2 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Cisplatin (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells. </p>

, 2013 , Dr. Edita Aksamitiene from Thomas Jefferson University

RH4 cells were stably transfected with STAT3-C vector. The expression of Flag-tagged STAT3 was examined in STAT3-C stably transfected RH4 and RH5 cells by western blot. (B) The inhibition of cell viability by cisplatin and doxorubicin in RH4 (B) cells was decreased in the presence of STAT3-C protein shown by MTT assay (*P<.05, ** P <.01, *** P <.001).

Gegevens van [ , , Curr Cancer Drug Targets, 2016, 16(7):631-8 ]

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.