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Plitidepsin
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。
Plitidepsin图片
CAS NO:137219-37-5
包装与价格:
包装价格(元)
500 µg电议
1mg电议

产品介绍
Plitidepsin (Aplidine) 是一种有效的抗癌剂,通过靶向 eEF1A2 (KD=80 nM)。
Cas No.137219-37-5
别名普拉泰,Aplidine
Canonical SMILESO=C1N2[C@](CCC2)([H])C(N([C@H](C(O[C@@H]([C@@H](C(N[C@]([C@H](CC(O[C@H](C([C@@H](C(N[C@H]1CC(C)C)=O)C)=O)C(C)C)=O)O)([H])[C@@H](C)CC)=O)NC([C@@H](CC(C)C)N(C)C([C@H]3N(C(C(C)=O)=O)CCC3)=O)=O)C)=O)CC4=CC=C(C=C4)OC)C)=O
分子式C57H87N7O15
分子量1110.3
溶解度DMSO: soluble
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Plitidepsin is a depsipeptide that was originally isolated fromAplidium albicansand has diverse biological activities.1,2,3It binds to the α subunit isoform eEF1A2 of eukaryotic elongation factor 1 (eEF1; Kd= 79 nM) and inhibits the proliferation of NCI H460 non-small cell lung cancer (NSCLC) and HGC-27 gastric cancer cells (IC50s = 0.2 and 0.9 nM, respectively).1Plitidepsin (0.01 nM) inhibits bone resorption by osteoclasts in a pit formation assay using bovine bone slices.2It reduces viral titers and lung inflammation in the K18-hACE2 mouse model of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection when administered at a dose of 0.3 mg/kg.3

1.Losada, A., MuÑoz-Alonso, M.J., GarcÍa, G., et al.Translation elongation factor eEF1A2 is a novel anticancer target for the marine natural product plitidepsinSci. Rep.635100(2016) 2.Delgado-Calle, J., Kurihara, N., Atkinson, E.G., et al.Aplidin (plitidepsin) is a novel anti-myeloma agent with potent anti-resorptive activity mediated by direct effects on osteoclastsOncotarget10(28)2709-2721(2019) 3.White, K.M., Rosales, R., Yildiz, S., et al.Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1AScience371(6532)926-931(2021)