Lobaplatin

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Lobaplatin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

135558-11-1

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
1mg	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议

产品名称

络铂
D-19466

产品介绍

Lobaplatin (D-19466) 是铂 (II) 络合物的非对映混合物。Lobaplatin 将细胞周期阻滞在 G1 和 G2/M 期。Lobaplatin 通过增加 caspase和 Bax 的表达，降低 Bcl-2 的表达来诱导细胞凋亡 (apoptosis)。Lobaplatin 可用于癌症研究。

生物活性

Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin inducesapoptosisby increasing expressions ofcaspaseandBax, decreasing expression ofBcl-2. Lobaplatin can be used for research ofcancer^[1]^[2]^[3].

体外研究
(In Vitro)

Lobaplatin (D-19466, 0.25-32 μg/mL; 24-72 h) exhibits anti-proliferative activities against esophageal squamous cell carcinoma (ESCC) cell lines^[1].
Lobaplatin (0-16 μg/mL; 48 h) induces esophageal squamous cell carcinoma (ESCC) apoptosis and modulates expression of apoptosis-related proteins^[1].
Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) arrests cell cycle progression at G1 and G2/M phases in a time-dependent manner^[2].
Lobaplatin (1.45 μg/mL; 0-48 h; SMMC-7721 cells) inhibits the mRNA levels of cyclin B, CDK1, and CDC25C phosphatase, down-regulates Rb/E2F complexes and up-regulates of CDK inhibitors^[2].

Cell Viability Assay^[1]

Cell Line:	KYSE-410 cells and EC-109 cells
Concentration:	0.25, 0.5, 1, 2, 4, 8, 16 and 32 μg/mL
Incubation Time:	24, 48 and 72 hours
Result:	Inhibited the growth of KYSE-410 and EC-109 cells in a dose- and time-dependent manner. Inhibited the clone formation activity of KYSE-410 and EC-109 cells in a dosedependent manner.

Apoptosis Analysis^[1]

Cell Line:	KYSE-410 cells and EC-109 cells
Concentration:	0.25, 1, 4 and 16 μg/mL
Incubation Time:	48 hours
Result:	Increased the percentage of apoptotic cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	KYSE-410 cells and EC-109 cells
Concentration:	0, 1, 4 and 16 μg/mL
Incubation Time:	48 hours
Result:	Increased expressions of cleaved-caspase-3, cleaved-caspase-8, cleaved-caspase-9 and Bax, while decreased expression of Bcl-2.

Cell Cycle Analysis^[2]

Cell Line:	SMMC-7721 cells
Concentration:	1.45 μg/mL
Incubation Time:	0, 24, 36 and 48 hours
Result:	Arrested the proportions of G1, S, and G2/M phases in cells were 45.31, 22.88, and 31.81% at 0 h, 59.91, 11.92, and 28.17% at 24 h, 56.89, 2.83, and 40.28% at 36 h, and 53.80, 2.07, and 44.13% at 48 h, respectively.

Western Blot Analysis^[2]

Cell Line:	SMMC-7721 cells
Concentration:	1.45 μg/mL
Incubation Time:	0, 24, 36 and 48 hours
Result:	Down-regulated cyclin B, CDK1, CDC25C, phosphorylated CDK1 (pCDK1), pCDK4, Rb, E2F, and pRb, and up-regulated p53, p21, and p27.

体内研究
(In Vivo)

Lobaplatin (5 and 10 mg/kg; i.p.; once a week, for 3 weeks) suppresses tumor growth of esophageal squamous cell carcinoma (ESCC) xenograft^[1].

Animal Model:	Male BALB/c nude mice (4-6 weeks) with ESCC xenograft^[1]
Dosage:	Intraperitoneal injection; once a week, for 3 weeks
Administration:	5 and 10 mg/kg
Result:	Suppressed tumor volumes in a dose-dependent manner. Increased expressions of Bax and decreased expressions of Bcl-2.

Clinical Trial

分子量

397.33

性状

Solid

Formula

C₉H₁₈N₂O₃Pt

CAS 号

135558-11-1

中文名称

络铂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : ≥ 50 mg/mL(125.84 mM;DMSO can inactivate Lobaplatin's activity)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.5168 mL	12.5840 mL	25.1680 mL
5 mM	0.5034 mL	2.5168 mL	5.0336 mL
10 mM	0.2517 mL	1.2584 mL	2.5168 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (251.68 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。