SM-276001

SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer^[1][2]. IC50 & Target: TLR7; IFN^[1][2] In Vitro: SM-276001 (1 nM-10 μM) dose-dependently activates NF-κB through human TLR7^[2]. In Vivo: SM-276001 demonstrates potent IFN-inducing activity at a dose of 0.1 mg/kg by oral administration in mice^[1].
Oral administration of SM-276001, leads to the induction of an inflammatory cytokine and chemokine milieu and to the activation of a diverse population of immune effector cells including T and B lymphocytes, NK and NKT cells^[2].
SM-276001 (3 mg/kg PO biweekly) significantly inhibits tumor growth in the Renca renal cell cancer and CT26 colorectal models^[2].
SM-276001 (orally; 0.1, 1 or 10 mg/kg) leads to the activation of a diverse population of spleen-resident immune effector cells in Balb/c and C57BL/6J mice. When administered at 1 mg/kg or greater, the plasma concentration of SM-276001 exceeds the MEC of 30 nM^[2].