SM-276001

• CAT Number: I016419
• CAS Number: 473930-22-2
• Molecular Formula: C16H21N7O
• Molecular Weight: 327.38
• Purity: ≥95%
• Synonyms: 6-amino-2-(butylamino)-9-[(6-methylpyridin-3-yl)methyl]-7H-purin-8-one
• InChI: InChI=1S/C16H21N7O/c1-3-4-7-18-15-21-13(17)12-14(22-15)23(16(24)20-12)9-11-6-5-10(2)19-8-11/h5-6,8H,3-4,7,9H2,1-2H3,(H,20,24)(H3,17,18,21,22)
• InChIKey: UEIOLEMXCBOQAX-UHFFFAOYSA-N
• SMILES: CCCCNC1=NC(=C2C(=N1)N(C(=O)N2)CC3=CN=C(C=C3)C)N

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].
SM-276001 (1 nM-10 μM) dose-dependently activates NF-κB through human TLR7[2].
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].

Reference

[1]. Isobe Y, et al. Synthesis and biological evaluation of novel 9-substituted-8-hydroxyadenine derivatives as potent interferon inducers. J Med Chem. 2006 Mar 23;49(6):2088-95.
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[2]. Koga-Yamakawa E, et al. Intratracheal and oral administration of SM-276001: a selective TLR7 agonist, leads to antitumor efficacy in primary and metastatic models of cancer. Int J Cancer. 2013 Feb 1;132(3):580-90.
 [Content Brief]