Miltefosine

Catalog No.S3056 Batch:S305602

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Technical Data

Formula

C21H46NO4P
Molecular Weight 407.57 CAS No. 58066-85-6
Solubility (25°C)* In vitro Water 81 mg/mL (198.73 mM)
Ethanol 81 mg/mL (198.73 mM)
DMSO Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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]
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]

Protocol (from reference)

Cell Assay:[6]
  • 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.

Animal Study: [6]
  • Animal Models

    BC-1 cells xenografted NOD-SCID mice

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Customer Product Validation

, , Biochem Biophys Res Commun, 2016, 469(4):1034-40.

, , Biochem Biophys Res Commun, 2016, 469(4):1034-40.

Selleck's Miltefosine has been cited by 13 publications

FAT10 Combined with Miltefosine Inhibits Mitochondrial Apoptosis and Energy Metabolism in Hypoxia-Induced H9C2 Cells by Regulating the PI3K/AKT Signaling Pathway [ Evid Based Complement Alternat Med, 2022, 2022:4388919] PubMed: 36034957
Bioanalytical methods for pharmacokinetic studies of antileishmanial drugs [ Biomed Chromatogr, 2022, e5519.] PubMed: 36208186
FOXM1-mediated activation of phospholipase D1 promotes lipid droplet accumulation and reduces ROS to support paclitaxel resistance in metastatic cancer cells [ Free Radic Biol Med, 2021, S0891-5849(21)00821-2] PubMed: 34808333
CORO1C is Associated With Poor Prognosis and Promotes Metastasis Through PI3K/AKT Pathway in Colorectal Cancer [ Front Mol Biosci, 2021, 8:682594] PubMed: 34179087
The PI3K/mTOR dual inhibitor GSK458 potently impedes ovarian cancer tumorigenesis and metastasis. [ Cell Oncol (Dordr), 2020, 8] PubMed: 32382996
Inhibition of MEIS3 Generates Cetuximab Resistance through c-Met and Akt [ Biomed Res Int, 2020, 2020:2046248] PubMed: 33376716
Protein Kinase B and Extracellular Signal-Regulated Kinase Inactivation is Associated with Regorafenib-Induced Inhibition of Osteosarcoma Progression In Vitro and In Vivo [ J Clin Med, 2019, 8(6)] PubMed: 31238539
LMO4 promotes the invasion and proliferation of gastric cancer by activating PI3K-Akt-mTOR signaling [ Am J Transl Res, 2019, 11(10):6534-6543] PubMed: 31737204
Functional Assessment of 2,177 U.S. and International Drugs Identifies the Quinoline Nitroxoline as a Potent Amoebicidal Agent against the Pathogen Balamuthia mandrillaris. [ mBio, 2018, 9(5)] PubMed: 30377287
Repurposing the quinoline antibiotic nitroxoline to treat infections caused by the brain-eating amoeba Balamuthia mandrillaris [ bioRxiv, 2018, 10.1101/331785] PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.