SM-276001
SM-276001 Basic information
- Product Name:
- SM-276001
- Synonyms:
-
- SM-276001
- immune,SM-276001,IFNAR,Interferon-alpha/beta receptor,IFN,Toll-like Receptor (TLR),SM276001,inhibit,TLR7,Inhibitor,Interferon-α/β receptor,interferon,SM 276001,antitumor
- 8H-Purin-8-one, 6-amino-2-(butylamino)-7,9-dihydro-9-[(6-methyl-3-pyridinyl)methyl]-
- SM-276001, 10 mM in DMSO
- 6-Amino-2-(butylamino)-9-((6-methylpyridin-3-yl)methyl)-7,9-dihydro-8H-purin-8-one
- CAS:
- 473930-22-2
- MF:
- C16H21N7O
- MW:
- 327.38
- Mol File:
- 473930-22-2.mol
SM-276001 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
SM-276001 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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