Plitidepsin Aplidine; PM90001|cas:137219-37-5|西域试剂

Plitidepsin Aplidine; PM90001,99.88%

产品编号：Bellancom-16050| CAS NO：137219-37-5| 分子式：C₅₇H₈₇N₇O₁₅| 分子量：1110.34

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16050	￥3600.00	杭州北京（现货）
Bellancom-16050	￥9000.00	杭州北京（现货）
Bellancom-16050	￥14200.00	杭州北京（现货）

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产品介绍

Plitidepsin (Aplidine) 是一种靶向 eEF1A2?(K_D=80 nM) 的有效抗癌活性分子。Plitidepsin 有抗病毒活性，抑制 SARS-CoV-2 的 IC₉₀ 为 0.88 nM。Plitidepsin 通常用于多发性骨髓瘤和晚期癌症研究，具有 COVID-19 研究的潜力。

生物活性

Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( K_D=80 nM). Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC₉₀ of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.

体外研究

Plitidepsin (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells.
Plitidepsin (20 nM; 1 h) does not result in significant inhibition of VEGF-R1 mRNA in normal endothelial cells, which do express VEGFR-1 but do not secrete VEGF.
Plitidepsin inhibits SARS-CoV-2 with an IC₉₀ of 1.76 nM. In hACE2-293T cells, Plitidepsin exhibits anti–SARS-CoV-2 activity with an IC₉₀ of 0.88 nM. In an established model of human pneumocyte-like cells, Plitidepsin inhibits SARS-CoV-2 replication with an IC₉₀ of 3.14 nM and a selectivity index of 40.4.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Plitidepsin (intraperitoneal injection; 0.3 mg/kg or 1 mg/kg; 2 hours before infection with SARS-CoV-2) significantly reduces SARS-CoV-2 infection in BALB/c mice expressing human ACE2. 0.3 mg/kg plitidepsin group results in a reduction of nearly 2 log units in SARS-CoV-2 viral titers in the lungs, and the 1 mg/kg group leads to a reduction of 1.5 log units relative to the vehicle control group.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c mice
Dosage:	0.3 mg/kg; 1 mg/kg
Administration:	1 day QD at 1 mg/kg; 3days QD at 0.3 mg/kg
Result:	Showed in vivo antiviral efficacy in mouse models of SARS-CoV-2 infection.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	BALB/c mice
Dosage:	0.3 mg/kg; 1 mg/kg
Administration:	1 day QD at 1 mg/kg; 3days QD at 0.3 mg/kg
Result:	Showed in vivo antiviral efficacy in mouse models of SARS-CoV-2 infection.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (90.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9006 mL	4.5031 mL	9.0063 mL
5 mM	0.1801 mL	0.9006 mL	1.8013 mL
10 mM	0.0901 mL	0.4503 mL	0.9006 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 (sealed storage, away from moisture and light, under nitrogen)。-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 (2.25 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (2.25 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

参考文献

. Alejandro Losada, et al. Translation Elongation Factor eEF1A2 is a Novel Anticancer Target for the Marine Natural Product Plitidepsin. Sci Rep. 2016 Oct 7;6:35100. [Content Brief]

. Kris M White, et al. Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A. Science. 2021 Feb 26;371(6532):926-931. [Content Brief]

化学品安全说明书(MSDS)

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Plitidepsin Aplidine; PM90001,99.88%

化学品安全说明书(MSDS)

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