Miltefosine
S3056
50mg~500mg
Brand
Selleckchem
Description
Miltefosine
Catalog No.S3056
Miltefosine 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. Phase 4.
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Biological Activity
| Description | Miltefosine 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. Phase 4. | |||||
|---|---|---|---|---|---|---|
| Targets | ||||||
| IC50 | ||||||
| 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] | |||||
| Features | ||||||
Protocol(Only for 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. |
| Solubility | Saline, 30 mg/mL |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators |
Start Date | Phases |
|---|---|---|---|---|---|
| NCT01377974 | Recruiting | Leishmaniasis|Leishmaniasis, Mucocutaneous | Brasilia University Hospital | 2010-01 | Phase 3 |
| NCT01067443 | Recruiting | Primary Visceral Leishmaniasis | Drugs for Neglected Diseases|Gilead Sciences|Paladin Laboratories Inc | 2010-03 | Phase 2 |
| NCT01050907 | Recruiting | Leishmaniasis, Mucocutaneous|Cutaneous Leishmaniasis | Paladin Labs (USA) Inc. | 2010-05 | Phase 2 |
| NCT01122771 | Recruiting | Visceral Leishmaniasis | Drugs for Neglected Diseases|Shaheed Surhawardy Medical College and Hospital|International Centre for Diarrhoeal Disease Research, Bangladesh | 2010-05 | Phase 3 |
| NCT01462500 | Not yet recruiting | Cutaneous Leishmaniasis | Centro Internacional de Entrenamiento e Investigaciones Mdicas|Academisch Medisch Centrum – Universiteit van Amsterdam (AMC-UvA) | 2011-10 | Phase 4 |
Chemical Information
| Molecular Weight (MW) | 407.57 |
|---|---|
| Formula |
C21H46NO4P |
| CAS No. | 58066-85-6 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | <1 mg/mL (<1 mM) |
|---|---|---|---|
| Water | 82 mg/mL (201 mM) | ||
| Ethanol | 82 mg/mL (201 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <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. |
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| Chemical Name | Ethanaminium, 2-[[(hexadecyloxy)hydroxyphosphinyl]oxy]-N,N,N-trimethyl-, inner salt |
|---|
Application
Reactivity
