SM-276001

Product NameSM-276001
CAS473930-22-2
MFC16H21N7O
MW327.38
EINECS
MOL File473930-22-2.mol

Chemical Properties

Melting point	248.5-252 °C(Solv: methanol (67-56-1))
Density	1.322±0.06 g/cm3(Predicted)
pka	10.30±0.20(Predicted)
form	Solid
color	Off-white to light yellow

Usage And Synthesis

Description

SM-276001 is a selective and potent TLR7 agonist. SM-276001 is can induce antitumor immune responses when dosed either intratracheally or orally. Oral administration of SM-276001 leads to the induction of IFNα, TNFα and IL-12p40 and a reduction in tumor burden in the Balb/c syngeneic Renca and CT26 models.

Uses

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].

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].

Animal Model:	C57BL/6 and B6C3F1 mice bearing Renca or CT26 tumors^[2]
Dosage:	3 mg/kg
Administration:	Oral administration twice weekly for 25 days
Result:	Significantly reduced disease burden in mice bearing either Renca or CT26 tumors.

References

[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. DOI:10.1021/jm051089s
[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. DOI:10.1002/ijc.27691

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