Cisplatin

Biological Activity

Cisplatin is an inorganic compound that is widely used for the treatment of a variety of tumors. Cisplatin induces apoptosis via p53-dependent and -independent mechanisms. Cisplatin inhibits X-linked inhibitor of apoptosis protein (XIAP) expression and activates caspase-3.

Product Citations

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  Bioengineered. 2021 Dec;12(1):2499-2510.

  Targeting the miR-6734-3p/ZEB2 axis hampers development of non-small cell lung cancer (NSCLC) and increases susceptibility of cancer cells to cisplatin treatment
  Cisplatin purchased from AbMole

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  2020 Dec.

  A Novel Circular RNA hsa_circRNA_103809/miR-377-3p/GOT1 Pathway Regulates Cisplatin-Resistance in Non-Small Cell Lung Cancer (NSCLC)
  Cisplatin purchased from AbMole

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  Open Life Sciences. 2020 June;15(1):409-417.

  Buformin suppresses osteosarcoma via targeting AMPK signaling pathway
  Cisplatin purchased from AbMole

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  Aging (Albany NY). 2020 Jun 9;12(11):11025-11041.

  LncRNA ADAMTS9-AS2 inhibits gastric cancer (GC) development and sensitizes chemoresistant GC cells to cisplatin by regulating miR-223-3p/NLRP3 axis
  Cisplatin purchased from AbMole

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  Cell Cycle. 2018;17(10):1235-1244.

  Apatinib, a novel tyrosine kinase inhibitor, suppresses tumor growth in cervical cancer and synergizes with Paclitaxel.
  Cisplatin purchased from AbMole

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  Cancer Biol Ther. 2018 Feb 5.

  Buformin suppresses proliferation and invasion via AMPK/S6 pathway in cervical cancer and synergizes with paclitaxel
  Cisplatin purchased from AbMole

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  J Korean Med Sci. 2016 Jun;31(6): 836–842.

  Silencing of ABCG2 by MicroRNA-3163 Inhibits Multidrug Resistance in Retinoblastoma Cancer Stem Cells
  Cisplatin purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Cell Cycle (2018 Jul). Figure 5. Cisplatin (Abmole Bioscience)
	Method	cellular proliferation assay
	Cell Lines	SiHa cells
	Concentrations	5 μM
	Incubation Time	-
	Results	However, we found no synergy between Apatinib and cisplatin (CI ranged from 1.149 to 5.647 in SiHa, CI ranged from 0.85 to 1.682 in Hcc94) or carboplatin (CI ranged from 0.669 to 1.402 in SiHa and from 0.955 to 1.206 in Hcc94)

	Source	Cancer Biol Ther (2018). Figure 6. cisplatin (Abmole Bioscience, Shanghai, China)
	Method	Buformin synergizes with chemotherapy
	Cell Lines	C33A cells
	Concentrations	1 μM
	Incubation Time
	Results	In C33A cells, low-dose buformin (1μM) significantly enhanced the anti-proliferative effects when combined with cisplatin, paclitaxel, or 5-FU

	Source	J Korean Med Sci (2016). Figure 5. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).
	Method	CCK8 Assay and ABCG2 ATPase assay
	Cell Lines	RCSC cells
	Concentrations	0~10 μM
	Incubation Time	72 h
	Results	MiR-3163 plays important roles in multidrug resistance (Table 1, Fig. 5A). Results showed that when miR-3163 was overexpressed in RCSCs, the ATPase activity of ABCG2 was significantly downregulated compared to RCSCs with Scramble (Fig. 5B).

	Source	J Korean Med Sci (2016). Figure 4. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).
	Method	CCK8 Assay and flow cytometry analysis
	Cell Lines	RCSC cells
	Concentrations	0~10 μM
	Incubation Time	72 h
	Results	"A lower proliferation rate was observed in RCSCs transfected with miR-3163 Mimics using the CCK-8 assay (Fig. 4A).RCSCs treated with miR-3163 Mimics were more susceptible to cisplatin-induced apoptosis compared to those treated with Scramble (Fig.4B)."

Protocol

Cell Experiment
Cell lines	A549-luc cell
Preparation method	Cells were allowed to adhere for 24 hours and subsequently incubated with either PRINT-Platin or cisplatin at concentrations ranging from 9.8 nM to 80 µM (drug concentration) for 72 hours at 37 °C in a humidified 5 % CO2 atmosphere. After the incubation period, all media/particles were aspirated off cells. 100 µL fresh medium was added back to cells, followed by the addition of 100 µL CellTiter-Glo® Luminescent Cell Viability Assay reagent.
Concentrations	9.8 nM to 80 µM
Incubation time	72 h

Animal Experiment
Animal models	healthy mice
Formulation	pH-adjusted 0.9 wt% NaCl solution
Dosages	3 mg/kg
Administration	vein injection

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

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

Evaluation of drug loading, pharmacokinetic behavior, and toxicity of a cisplatin-containing hydrogel nanoparticle.
Kai MP, et al. J Control Release. 2015 Apr 28;204:70-7. PMID: 25744827.

Mechanism of cisplatin proximal tubule toxicity revealed by integrating transcriptomics, proteomics, metabolomics and biokinetics.
Wilmes A, et al. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):117-27. PMID: 25450742.

Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes
Matthew D Hall, et al. Cancer Res. 2014 Jul 15;74(14):3913-22. PMID: 24812268.