A TLR7 agonist
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852A

Item No. 39512

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]-methanesulfonamide
CAS Number
532959-63-0
Synonyms
  • PF-4878691
Molecular Formula
C17H23N5O2S
Formula Weight
361.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): Slightly soluble
SMILES
NC(C1=C2N(CCCCNS(C)(=O)=O)C(CC)=N1)=NC3=C2C=CC=C3
InChi Code
InChI=1S/C17H23N5O2S/c1-3-14-21-15-16(12-8-4-5-9-13(12)20-17(15)18)22(14)11-7-6-10-19-25(2,23)24/h4-5,8-9,19H,3,6-7,10-11H2,1-2H3,(H2,18,20)
InChi Key
YZOQZEXYFLXNKA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    852A is a toll-like receptor 7 (TLR7) agonist.1 It selectively induces NF-κB signaling in HEK293 cells expressing recombinant human TLR7 but not HEK293 cells expressing recombinant human TLR8 or TLR9 when used at a concentration of 1 µM. 852A (10-1,000 ng/ml) also induces IFN-α production in plasmacytoid dendritic cell-enriched but not plasmacytoid dendritic cell-depleted isolated human peripheral blood mononuclear cells (PBMCs). In vivo, 852A (150 mg/kg) delays the onset of lung metastasis in a B16/F10 murine melanoma model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dudek, A.Z., Yunis, C., Harrison, L.I., et al. First in human phase I trial of 852A, a novel systemic toll-like receptor 7 agonist, to activate innate immune responses in patients with advanced cancer. Clin. Cancer Res. 13(23), 7119-7125 (2007).

    2. Inglefield, J.R., Dumitru, C.D., Alkan, S.S., et al. TLR7 agonist 852A inhibition of tumor cell proliferation is dependent on plasmacytoid dendritic cells and type I IFN. J. Interferon Cytokine Res. 28(4), 253-263 (2008).