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: 58066-85-6

Selleck's Miltefosine has been cited by 13 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: >97%
97

Other Akt Products

Related compound libraries

Choose Selective Akt Inhibitors

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 lnformation & 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.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Miltefosine | Miltefosine supplier | purchase Miltefosine | Miltefosine cost | Miltefosine manufacturer | order Miltefosine | Miltefosine distributor