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Aplidine

Catalog No. T9715   CAS 137219-37-5

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).

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Aplidine Chemical Structure
Aplidine, CAS 137219-37-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 297.00
5 mg In stock $ 728.00
10 mg In stock $ 987.00
25 mg In stock $ 1,530.00
50 mg In stock $ 1,980.00
1 mL * 10 mM (in DMSO) In stock $ 1,330.00
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Purity: 98.12%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).
Targets&IC50 eEF1A2:80 nM(Kd), SARS-CoV-2:0.88 nM(IC90)
In vitro 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]. Aplidine (20 nM; 1 h) induces a dose-dependent decrease in VEGF secretion in MOLT-4 cells. 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].
In vivo In BALB/c mice expressing human ACE2, Aplidine significantly reduced SARS-CoV-2 infection. 0.3 mg/kg Aplidine 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[2].
Molecular Weight 1110.34
Formula C57H87N7O15
CAS No. 137219-37-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (90.06 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library

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Keywords

Aplidine 137219-37-5 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology SARS-CoV DNA/RNA Synthesis Inhibitor MOLT-4 SARS coronavirus infection Plitidepsin Leukemia VEGF COVID-19 Antiviral inhibit advanced cancer anticancer Advanced Malignancies inhibitor

 

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