product name Miltefosine
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. When tested with macrophages infected by human HIV-1 virus, miltefosine showed significant ability to reduce the viral production via inhibiting PI3K/Akt signaling pathway. In L6E9 skeltal muscle cell line, treatment of milefosine resulted in the resistance of skeletal muscle cells via inhibiting PI3K/Akt signaling pathway。
References: Br J Cancer. 2001 May 18;84(10):1405-11.
407.57
Formula
C21H46NO4P
CAS No.
58066-85-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 82 mg/mL (201.2 mM)
Ethanol: 82 mg/mL (201.2 mM)
Solubility (In vivo)
Saline: 30mg/mL
Chemical Name
hexadecyl 2-(trimethylazaniumyl)ethyl phosphate
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394332
| In Vitro | Kinase Assay:
Cell Assay: 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. 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. 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. Miltefosine inhibits the PI3K/Akt survival pathway in carcinoma cell lines. 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. |
|---|---|
| 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 |
| Animal model | BC-1 cells xenografted NOD-SCID mice |
| Formulation & Dosage | Formulated inPBS; 50 mg/kg; i.p. |
| References | [1] Meuillet EJ, et al. Mol Cancer Ther, 2010, 9(3), 706-717. |
Related Posts
product name Miltefosine
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. When tested with macrophages infected by human HIV-1 virus, miltefosine showed significant ability to reduce the viral production via inhibiting PI3K/Akt signaling pathway. In L6E9 skeltal muscle cell line, treatment of milefosine resulted in the resistance of skeletal muscle cells via inhibiting PI3K/Akt signaling pathway。
References: Br J Cancer. 2001 May 18;84(10):1405-11.
407.57
Formula
C21H46NO4P
CAS No.
58066-85-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: <1 mg/mL
Water: 82 mg/mL (201.2 mM)
Ethanol: 82 mg/mL (201.2 mM)
Solubility (In vivo)
Saline: 30mg/mL
Chemical Name
hexadecyl 2-(trimethylazaniumyl)ethyl phosphate
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394332
| In Vitro | Kinase Assay:
Cell Assay: 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. 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. 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. Miltefosine inhibits the PI3K/Akt survival pathway in carcinoma cell lines. 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. |
|---|---|
| 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 |
| Animal model | BC-1 cells xenografted NOD-SCID mice |
| Formulation & Dosage | Formulated inPBS; 50 mg/kg; i.p. |
| References | [1] Meuillet EJ, et al. Mol Cancer Ther, 2010, 9(3), 706-717. |