gardiquimod

Description: Gardiquimod DiTFA salt is a novel, potent and specific TLR7 (toll-like receptor 7) agonist which can also inhibit HIV-1 reverse transcriptase. Gardiquimod can promote the proliferation of murine splenocytes, stimulate the activation of splenic T, NK and natural killer T (NKT) cells, increase the cytolytic activity of splenocytes against B16 and MCA-38 tumor cell lines, and enhance the expression of costimulatory molecules and IL-12 by macrophages and bone marrow-derived dendritic cells (DCs). In a murine model, Gardiquimod improved the antitumor effects of tumor lysate-loaded DCs, resulting in delayed growth of subcutaneous B16 melanoma tumors and suppression of pulmonary metastasis. Gardiquimod demonstrated more potent antitumor activity than imiquimod. These results suggest that TLR7/8 agonists such as Gardiquimod may serve as potent innate and adaptive immune response modifiers in tumor therapy. More importantly, they can be used as vaccine adjuvants to potentiate the efficiency of DC-based tumor immunotherapy.

References: Cell Mol Immunol. 2010 Sep; 7(5):381-8.

Related CAS #: 1159840-61-5 (TFA) 1020412-43-4 (free base)