Details
Stereochemistry | ACHIRAL |
Molecular Formula | C36H59N5O2 |
Molecular Weight | 593.886 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCCCCCCCCCCCCCC(=O)NCCCCON1C(CCCC)=NC2=C1C3=C(C=CC=C3)N=C2N
InChI
InChIKey=RRTPWQXEERTRRK-UHFFFAOYSA-N
InChI=1S/C36H59N5O2/c1-3-5-7-8-9-10-11-12-13-14-15-16-17-18-19-27-33(42)38-28-22-23-29-43-41-32(26-6-4-2)40-34-35(41)30-24-20-21-25-31(30)39-36(34)37/h20-21,24-25H,3-19,22-23,26-29H2,1-2H3,(H2,37,39)(H,38,42)
MedImmune is developing MEDI 9197 (formerly 3M-052), a toll-like receptor 7/8 dual agonist, for the treatment of cancer. MEDI9197 has been designed to activate a broad range of innate immune cells through targeting of both TLR 7 and 8, leading to a more robust adaptive immune response. A TLR7 and 8 dual agonist can additionally convert immune suppressive cells in the tumor to those with anti-tumor properties, allowing the generation of an effective anti-tumor response. MEDI9197 is uniquely designed for intratumoral injection, allowing the compound to be retained in the tumor and provide specific immune activation, enhancing its safety and tolerability profile.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Combination therapy targeting toll like receptors 7, 8 and 9 eliminates large established tumors. | 2014 |
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Adsorption of a synthetic TLR7/8 ligand to aluminum oxyhydroxide for enhanced vaccine adjuvant activity: A formulation approach. | 2016 Dec 28 |
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Adjuvant composition and delivery route shape immune response quality and protective efficacy of a recombinant vaccine for Entamoeba histolytica. | 2018 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24982761
Mice: CT26 colon cancer cells were implanted subcutaneouslyinto the flank of syngeneic BALB/c mice. When these tumors reached 200 mm3 in volume, 100 ug of ODN and/or 50 ug of 3M-052 was injected intra-tumorally and the procedure repeated 2 days later.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28804955
In vitro stimulation of bone marrow-derived dendritic cells, measured by IL-12 secretion, demonstrated that 3M-052 (free or MP-formulated) had a concentration-dependent immunostimulatory effect with an optimum concentration of 2 ug/mL.
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C2139
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ACTIVE MOIETY