Mito-LND - CAS:2361564-49-8

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Mito-LND (Synonyms:Mito-Lonidamine)

目录号 : KM3562 CAS No. : 2361564-49-8 纯度 : 97%

Data Sheet 产品使用指南

Mito-LND (Mito-Lonidamine) 是一种具有口服活性的且靶向线粒体的氧化磷酸化 (oxidative phosphorylation (OXPHOS)) 抑制剂。Mito-LND 抑制线粒体生物能，刺激活性氧 (reactive oxygen species) 的形成，并诱导肺癌细胞自噬细胞死亡。

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10mg		In-stock
25mg		In-stock
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500mg	询价	In-stock

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生物活性

Mito-LND (Mito-Lonidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation (OXPHOS). Mito-LND inhibits mitochondrial bioenergetics, stimulates the formation of reactive oxygen species, and induces autophagic cell death in lung cancer cells.

体外研究

Mito-LND blocks lung cancer growth, migration, and invasion. Mito-LND inhibits cell growth of H2030BrM3 and A549 cells with IC₅₀ values of 0.74 µM and 0.69 µM, respectively.
Mito-LND inhibits mitochondrial complex I and II activities with IC₅₀ values of 1.2 µM and 2.4 µM, respectively in H2030BrM3 cells.
Mito-LND (1 µM) increases ROS generation in H2030BrM3 lung cancer cells. Mito-LND potently induces mitochondrial ROS generation in H2030BrM3 lung cancer cells.
Mito-LND (2 µM) decreases the levels of phosphorylated AKT. Mito-LND also decreases the phosphorylation of P70S6K and other energy-sensing proteins in both the parental and metastatic lung cancer cell lines, indicating that Mito-LND specifically downregulates mTOR signaling.

体内研究

Mito-LND (7.5 µmol/kg; oral gavage; 5 days per week; for 3 consecutive weeks) treatment markedly enhanced potency against both lung cancer progression and metastasis.
Mito-LND also decreases the rate of growth of A549 tumor xenografts.
Mito-LND treatment shows a marked decrease in lung cancer brain metastasis in NOD/SCID mice bearing H2030BrM3 cells.

Animal Model:	Athymic nude mice (5 weeks) injected with H2030BrM3 cells
Dosage:	7.5 µmol/kg
Administration:	Oral gavage; 5 days per week; for 3 consecutive weeks
Result:	Significantly decreased tumor progression.

分子式

C₄₃H₄₅BrCl₂N₃OP

分子量

801.62

CAS号

2361564-49-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 50 mg/mL (62.37 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2475 mL	6.2374 mL	12.4747 mL
5 mM	0.2495 mL	1.2475 mL	2.4949 mL
10 mM	0.1247 mL	0.6237 mL	1.2475 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (3.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。