Plitidepsin|137219-37-5|(Aplidine; PM90001)-陌孚医药/Medlife

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Plitidepsin (Synonyms: Aplidine; PM90001)

目录号: PL11165 纯度: ≥99%

CAS No. :137219-37-5

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PL11165-50mg	50mg	询价	询价
PL11165-100mg	100mg	询价	询价

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中文名称	Plitidepsin
英文名称	Plitidepsin
英文别名	Didemnin A,N-[1-(1,2-dioxopropyl)-L-prolyl]-;Plitidepsin;2-9-Didemnin B, 2-(1-(1,2-dioxopropyl)-L-proline)-;Aplidin;Aplidine;Dehydrodidemnin B;Didemnin A, N-(1-(1,2-dioxopropyl)-L-prolyl)-;L-Tyrosine, 1-(1,2-dioxopropyl)-L-prolyl-N-methyl-D-leucyl-L-threonyl-(3S,4R,5S)-4-amino-3-hydroxy-5-methylheptanoyl-(2S,4S)-4-hydroxy-2,5-dimethyl-3-oxohexanoyl-L-leucyl-L-prolyl-N,O-dimethyl-, (8-3)-lactone;Y76ID234HW;Plitidepsin [INN:BAN];plitidepsina;plitidepsine;plitidepsium;Plit
Cas No.	137219-37-5
分子式	C₅₇H₈₇N₇O₁₅
分子量	1110.34
包装储存	Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

产品详情

Plitidepsin (Aplidine) 是一种靶向 eEF1A2 (K_D=80 nM) 的有效抗癌药物。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 IC 90 of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.

性状

Solid

体外研究(In Vitro)

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

体内研究(In Vivo)

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

ClinicalTrial

结构分类

Alkaloids Pyrrole

参考文献

[1]. 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.
[2]. 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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (90.06 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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