Home PI3K/Akt/mTOR Akt inhibitor Miltefosine

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Miltefosine Akt inhibitor

Cat.No.S3056

Miltefosine (Hexadecylphosphocholine) inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, and is the first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
Miltefosine Akt inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 407.57

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

Water : 82 mg/mL

Ethanol : 82 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 407.57 Formula

C21H46NO4P

 Storage (From the date of receipt)
CAS No. 58066-85-6 Download SDF Storage of Stock Solutions

Synonyms Hexadecylphosphocholine Smiles CCCCCCCCCCCCCCCCOP(=O)([O-])OCC[N+](C)(C)C

Mechanism of Action

Targets/IC50/Ki
Akt
PI3K
PKC
~7 μM
In vitro
Miltefosine is an alkylphosphocholine drug with demonstrated activity against various parasite species and cancer cells as well as some pathogenic bacteria and fungi. This compound inhibits PKC from NIH3T3 cells in cell-free extracts with a IC50 of about 7 μM. It targets HIV infected macrophages, which play a role in vivo as long-lived HIV-1 reservoirs. This chemical acts by inhibiting the PI3K/Akt pathway, thus removing the infected macrophages from circulation, without affecting healthy cells. It inhibits the PI3K/Akt survival pathway in carcinoma cell lines. This compound causes skeletal muscle insulin resistance in vitro by interfering with the insulinsignalling pathway and inhibiting insulin-stimulated glucose uptake. It inhibits insulin-stimulated Akt phosphorylation in a dose-dependent manner with 75% inhibition at 40 μM and 98% inhibition at 60 μM.
In vivo
Miltefosine inhibits anti-IgE induced histamine release from human skin mast cells. This compound can reduce cytokines IL-1β, IL-4, and IL-6 in certain skin tissue cells and also strongly impede the esterification of cholesterol.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16752184/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19917276/
  • [6] https://pubmed.ncbi.nlm.nih.gov/20299510/

Applications

Methods Biomarkers Images PMID
Western blot p-AMPKα / AMPKα / p-ACC / ACC / p-IRS2 / IRS2 / p-SREBP1C / SREBP1C p-AKT / AKT / VEGF / MMP-9 / XIAP / Cyclin D1 / MCL-1 / C-FLIP
S3056-WB1
27681040

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05493059 Not yet recruiting
Cutaneous Leishmaniases|Treatment Adherence|Primary Health Care|Drug Evaluation
Centre Hospitalier de Cayenne
 August 8 2022 --
NCT03399955 Unknown status
PKDL - Post-Kala-Azar Dermal Leishmanioid
Drugs for Neglected Diseases
 May 9 2018 Phase 2
NCT02193022 Completed
Post Kala Azar Dermal Leishmaniasis
International Centre for Diarrhoeal Disease Research Bangladesh|Thrasher Research Fund
 July 2014 Phase 3
NCT01462500 Completed
Cutaneous Leishmaniasis
Centro Internacional de Entrenamiento e Investigaciones Médicas|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)
 October 2011 Phase 4

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