Molecular Weight(MW): 458.6
Motolimod (VTX-2337) is a selective and potent Toll-like receptor (TLR) 8 agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
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|Description||Motolimod (VTX-2337) is a selective and potent Toll-like receptor (TLR) 8 agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.|
VTX-2337 stimulates the production of both TNFα with EC50 of 140 nM and IL-12 with EC50 of 120 nM in PBMCs. In monocytes and mDCs, VTX-2337 selectively induces the production of TNFα and IL-12 via NF-κB activation. VTX-2337 also stimulates IFNγ production from NK cells, augments the lytic function of NK cells and enhances ADCC. 
|In vivo||In an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD). |
Activity assay:The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate (InvivoGen) after TLR agonist treatment is carried out.
|In vitro||DMSO||55 mg/mL warmed (119.93 mM)|
|Ethanol||15 mg/mL (32.7 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03906526||Recruiting||Drug: VTX-2337|Drug: Nivolumab||Carcinoma Squamous Cell||Celgene||July 3 2019||Phase 1|
|NCT01289210||Terminated||Drug: VTX-2337 plus radiotherapy||Low Grade B Cell Lymphoma||Celgene|Stanford University||July 2011||Phase 1|Phase 2|
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