Home PI3K/Akt/mTOR Akt inhibitor Miltefosine For research use only.

Miltefosine

Synonyms: Hexadecylphosphocholine

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

Miltefosine Chemical Structure

Miltefosine Chemical Structure

CAS No. 58066-85-6

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Miltefosine Related Products

Signaling Pathway

Akt Signaling Pathways

Akt Signaling Pathway

Biological Activity

Description Miltefosine (Hexadecylphosphocholine) inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
Targets
Akt [2] PI3K [2] PKC [1]
~7 μM
In vitro
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. Miltefosine inhibits PKC from NIH3T3 cells in cell-free extracts with a IC50 of about 7 μM.[1] Miltefosine targets HIV infected macrophages, which play a role in vivo as long-lived HIV-1 reservoirs. Miltefosine acts by inhibiting the PI3K/Akt pathway, thus removing the infected macrophages from circulation, without affecting healthy cells.[2] Miltefosine inhibits the PI3K/Akt survival pathway in carcinoma cell lines.[3] Miltefosine causes skeletal muscle insulin resistance in vitro by interfering with the insulinsignalling pathway and inhibiting insulin-stimulated glucose uptake. Miltefosine inhibits insulin-stimulated Akt phosphorylation in a dose-dependent manner with 75% inhibition at 40 μM and 98% inhibition at 60 μM.[4]
Cell Research Cell lines BCLM, VG-1, BC-1, and BCBL-1 PEL cell lines
Concentrations 10, 20, 30, 40, and 50μM
Incubation Time 3 days
Method 2 × 105 PEL cells are treated with the therapeutic compounds at the indicated doses or with appropriate vehicle as a negative control. Cells are followed for 96 hours, and cell viability is determined by trypan blue exclusion performed in quadruplicate.
Experimental Result Images 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 27681040
In Vivo
In vivo Miltefosine inhibits anti-IgE induced histamine release from human skin mast cells. Miltefosine can reduce cytokines IL-1β, IL-4, and IL-6 in certain skin tissue cells and also strongly impede the esterification of cholesterol. [5]
Animal Research Animal Models BC-1 cells xenografted NOD-SCID mice
Dosages 50 mg/kg
Administration i.p.
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

Chemical Information & Solubility

Molecular Weight 407.57 Formula

C21H46NO4P
CAS No. 58066-85-6 SDF Download Miltefosine SDF
Smiles CCCCCCCCCCCCCCCCOP(=O)([O-])OCC[N+](C)(C)C
Storage (From the date of receipt)

In vitro
Batch:

Water : 82 mg/mL

Ethanol : 82 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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