Cisplatin 顺铂

生物活性

Cisplatin是一种无机的铂络合物，通过形成DNA交联剂抑制DNA合成。Cisplatin 通过与DNA相互作用形成DNA交联剂诱导细胞毒性，激活多条信号转导通路, 包括Erk, p53, p73, 和MAPK,其中对激活凋亡影响最大。 Cisplatin (30 mM) 处理 HeLa 细胞6小时，显著激活Erk，持续到随后的14个小时期间。Cisplatin 还具有有效的抗肿瘤活性，诱导肿瘤细胞死亡。

DMSO会破坏顺铂的活性！

使用AbMole产品发表的文献

• Molecules. 2023 Mar 16;28(6):2685.

  Chemical Constituents of Thesium chinense Turcz and Their In Vitro Antioxidant, Anti-Inflammatory and Cytotoxic Activities

• J Immunother Cancer. 2022 Oct;10(10):e005270.

  CUL3/SPOP complex prevents immune escape and enhances chemotherapy sensitivity of ovarian cancer cells through degradation of PD-L1 protein

• Sci Rep. 2022 Oct 17;12(1):17358.

  Screening of the siGPCR library in combination with cisplatin against lung cancers

• Phytochemistry. 2022 Dec 12;207:113558.

  Diverse alkaloids from the aerial parts of Aconitum carmichaelii and antiproliferative activity of costemline via inhibiting SIRT1/ROCK1/P-STAT3 pathways

• Evid Based Complement Alternat Med. 2022 Apr 6;2022:4445293.

  Zhenzhu Xiaoji Decoction Induces Autophagy and Apoptosis Cell Death in Liver Cancer Cells through AKT/mTOR and JAK2/STAT3 Signaling Pathway

• Clin Epigenetics. 2021 Jul 22;13(1):142.

  Genome-wide DNA methylome analysis identifies methylation signatures associated with survival and drug resistance of ovarian cancers

• 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

• 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

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

  Buformin suppresses osteosarcoma via targeting AMPK signaling pathway

• 2020 Dec.

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

• Cell Cycle. 2018;17(10):1235-1244.

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

• Cancer Biol Ther. 2018 Feb 5.

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

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

  Silencing of ABCG2 by MicroRNA-3163 Inhibits Multidrug Resistance in Retinoblastoma Cancer Stem Cells

产品使用成果展示

	数据来源	Cell Cycle (2018 Jul). Figure 5. Cisplatin (Abmole Bioscience)
	方法	cellular proliferation assay
	细胞系/动物模型	SiHa cells
	浓度	5 μM
	处理时间	-
	实验结果	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)

	数据来源	Cancer Biol Ther (2018). Figure 6. cisplatin (Abmole Bioscience, Shanghai, China)
	方法	Buformin synergizes with chemotherapy
	细胞系/动物模型	C33A cells
	浓度	1 μM
	处理时间
	实验结果	In C33A cells, low-dose buformin (1μM) significantly enhanced the anti-proliferative effects when combined with cisplatin, paclitaxel, or 5-FU

	数据来源	J Korean Med Sci (2016). Figure 5. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).
	方法	CCK8 Assay and ABCG2 ATPase assay
	细胞系/动物模型	RCSC cells
	浓度	0~10 μM
	处理时间	72 h
	实验结果	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).

	数据来源	J Korean Med Sci (2016). Figure 4. cisplatin, mitoxantrone and topotecan were all purchased from AbMole BioScience (Shanghai, China).
	方法	CCK8 Assay and flow cytometry analysis
	细胞系/动物模型	RCSC cells
	浓度	0~10 μM
	处理时间	72 h
	实验结果	"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)."

实验参考

体外实验*
细胞系	A549-luc cell
方法	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.
浓度	9.8 nM to 80 µM
处理时间	72 h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	healthy mice
配制	pH-adjusted 0.9 wt% NaCl solution
剂量	3 mg/kg
给药处理	vein injection

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	300.05
分子式	Cl2H6N2Pt
CAS号	15663-27-1
溶解性（25°C）	DMF: 6 mg/mL (Need ultrasonic)
储存条件	2-8°C, protect from light
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.3328 mL	16.6639 mL	33.3278 mL
5 mM	0.6666 mL	3.3328 mL	6.6656 mL
10 mM	0.3333 mL	1.6664 mL	3.3328 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Kai MP, et al. J Control Release. Evaluation of drug loading, pharmacokinetic behavior, and toxicity of a cisplatin-containing hydrogel nanoparticle.

[2] Wilmes A, et al. Toxicol In Vitro. Mechanism of cisplatin proximal tubule toxicity revealed by integrating transcriptomics, proteomics, metabolomics and biokinetics.

[3] Matthew D Hall, et al. Cancer Res. Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes