| Description | Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7. |
| In vitro | VTX-2337 induces the production of both TNFα (EC50: 140 nM) and IL-12 (EC50: 120 nM) in PBMCs. In mDCs and monocytes, VTX-2337 specifically induces the production of IL-12 and TNFα via NF-κB activation. VTX-2337 also induces IFNγ production from NK cells, enhances the lytic function of NK cells and augments ADCC. |
| In vivo | In ovarian cancer mouse model, TX-2337 augments the effect of pegylated liposomal doxorubicin (PLD). |
| Cell experiments | PBMCs or purified NK cells are prepared as previously described, and the purity of NK cells was approximately 99%. NK cell-mediated cytotoxicity is assessed by Calcein-AM release from labeled target cells. In brief, PBMCs or purified NK cells are cultured for 48 hours in RPMI medium in the presence of VTX-2337 (167 or 500 nmol/L) before incubation with target cells. |
| Target activity | TLR8:100 nM(EC50) |
| Synonyms | VTX-378, VTX-2337 |
| molecular weight | 458.6 |
| Molecular formula | C28H34N4O2 |
| CAS | 926927-61-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 12 mg/mL (26.2 mM) DMSO: 51 mg/mL (111.2 mM) |
| References | 1. Lu H, et al. Clin Cancer Res. 2012, 18(2), 499-509. 2. Monk BJ, et al. J Clin Oncol 31, 2013 (suppl; abstr 3077). |
| Citations | 1. Yang W, Sun X, Liu S, et al.TLR8 agonist Motolimod-induced inflammatory death for treatment of acute myeloid leukemia.Biomedicine & Pharmacotherapy.2023, 163: 114759. |