| MDL | - |
|---|---|
| Molecular Weight | 1351.52 |
| Molecular Formula | C61H110F3N6O21P |
| SMILES | CCCCCCCCCCCCCCCC(OC[C@@H](OC(CCCCCCCCCCCCCCC)=O)COP(OCCNC([C@@H](NC(CC[C@@H](NC([C@@H](NC([C@H](O[C@]([C@H](O)[C@H](O)CO)([H])[C@@H](NC(C)=O)C=O)C)=O)C)=O)C(N)=O)=O)C)=O)(O)=O)=O.OC(C(F)(F)F)=O |
Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide TFA has the potential for osteosarcoma research [1] [2] [3] .
|
NOD2 |
Mifamurtide TFA (MTP-PE TFA; 100 µM) induces a reduction of MG63 cells number when co-cultured with macrophages
[3]
.
Mifamurtide TFA (100 µM) increases both the M1 polarization marker iNOS and the M2 polarization marker CD206 mRNAs; both pro-inflammatory (IL-1β, IL-6) and anti-inflammatory (IL-4, IL-10) cytokines. Mifamurtide TFA increases the iron transporter DMT1 protein
[3]
.
L-mifamurtide TFA (5, 5000 nM; for 48 hours) alone has no direct effect on the proliferation rate of the two osteosarcoma cell lines MOS-J and KHOS in vitro or in vivo
[1]
.
Mifamurtide TFA acts as a nonspecific immunomodulator by activating macrophages and monocytes related to the upregulation of tumoricidal activity and secretion of pro-inflammatory cytokines including tumor necrosis factor (TNF)-a, interleukin (IL)-1, IL-6, IL-8, IL-12, nitric oxide (NO), prostaglandin E2 (PGE2) and PGD2
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Mifamurtide TFA (MTP-PE TFA; 1 mg/kg; i.v.; twice per week for 4 weeks) causes a trend of diminished spontaneous lung metastasis dissemination
[1]
.
Mifamurtide TFA (50 μg/mouse) improves glucose tolerance during endotoxemia in mice. Mifamurtide TFA (equivalent to 20 μg MDP; 4 times per week for 5 weeks) improves glucose tolerance in HFD-fed mice without altering body mass
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6, BALB/c mice with KHOS osteosarcoma cells [1] |
| Dosage: | 1 mg/kg |
| Administration: | IV; twice per week for 4 weeks |
| Result: | Caused a trend of diminished spontaneous lung metastasis dissemination in xenogeneic (KHOS) and syngeneic (MOS-J) models. |
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03643133 | UNICANCER |
Osteosarcoma
|
October 23, 2018 | Phase 2 |
| NCT02441309 | University of Oxford|Millennium: The Takeda Oncology Company|National Institute for Health Research, United Kingdom|Oxford University Hospitals NHS Trust|European Commission |
Osteosarcoma
|
October 2014 | Phase 2 |
| NCT00631631 | Millennium Pharmaceuticals, Inc. |
Osteosarcoma
|
January 2008 | |
| NCT04571229 | Memorial Sloan Kettering Cancer Center |
Osteosarcoma
|
||
| NCT01194284 | Millennium Pharmaceuticals, Inc.|Takeda |
Osteosarcoma
|
December 2011 | |
| NCT01459484 | Italian Sarcoma Group |
Osteosarcoma
|
June 23, 2011 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 25 mg/mL ( 18.50 mM ; ultrasonic and warming and heat to 60°C)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.7399 mL | 3.6995 mL | 7.3991 mL |
| 5 mM | 0.1480 mL | 0.7399 mL | 1.4798 mL |
| 10 mM | 0.0740 mL | 0.3700 mL | 0.7399 mL |