Aplidine|CAS 137219-37-5|DC Chemicals

Cas No.:	137219-37-5
Chemical Name:	Didemnin A,N-[1-(1,2-dioxopropyl)-L-prolyl]-
SMILES:	COC1=CC=C(C=C1)CC2N(C)C(=O)[C@H]3N(CCC3)C(=O)[C@H](CC(C)C)NC(=O)[C@H](C)C(=O)[C@H](C(C)C)OC(=O)C[C@H](O)C([C@@H](C)CC)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@H]4N(CCC4)C(=O)C(C)=O)[C@H](C)OC2=O
Formula:	C₅₇H₈₇N₇O₁₅
M.Wt:	1110.33858
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Aplidine (Plitidepsin) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM)[1]. Aplidine possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Aplidine is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research[1][2].
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[2]. Animal Model: BALB/c mice[1] 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.
In Vitro:	Aplidine (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells[1]. Aplidine (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[1]. Aplidine inhibits SARS-CoV-2 with an IC90 of 1.76 nM. In hACE2-293T cells, Aplidine exhibits anti–SARS-CoV-2 activity with an IC90 of 0.88 nM. In an established model of human pneumocyte-like cells, Aplidine inhibits SARS-CoV-2 replication with an IC90 of 3.14 nM and a selectivity index of 40.4[1].
References:	[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.

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