PF-4878691

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Chemical Structure| 532959-63-0 同义名 : 3M-852A
CAS号 : 532959-63-0
货号 : A611478
分子式 : C17H23N5O2S
纯度 : 99%+
分子量 : 361.462
MDL号 : MFCD30533308
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(49.8 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The recognition of viral single‐stranded RNA by Toll‐like receptor 7 (TLR7) had been shown to induce an antiviral response in the host against hepatitis C virus (HCV). PF-4878691 is a potent and selective TLR7 agonist. It activated nuclear factor-κB in HEK293 cells transfected with TLR7 at a concentration of >3.3μmol/L. PF-4878691 induced the production of interferon (IFN)-α from human peripheral blood mononuclear cells (PBMCs) at a concentration of 0.041μmol/L. The stimulation of PBMCs with PF-4878691 also led to the activation of natural killer cells[1]. The supernatants from PBMCs stimulated with 0.1μM PF-4878691 inhibited the proliferation of tumor cell lines Hs294T and 769-P. PF-4878691 at low nanomolar concentrations (≥0.04μM) stimulated the production of IFN-inducible protein-10, interleukin (IL)-1 receptor antagonist, monocyte chemotactic protein-1, and tumor necrosis factor-related apoptosis-inducing ligand from human PBMCs. PF-4878691 at 3–30μM also induced the production of IL-12p70, IL-18, and IFN-γ. In a B16 melanoma mouse model, six oral doses of PF-4878691 (150mg/kg, every other day) significantly delayed the onset of lung colonies[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.67mL

5.53mL

2.77mL
参考文献

[1]Dudek AZ, Yunis C, Harrison LI, Kumar S, Hawkinson R, Cooley S, Vasilakos JP, Gorski KS, Miller JS. 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. 2007 Dec 1;13(23):7119-25.

[2]Inglefield JR, Dumitru CD, Alkan SS, Gibson SJ, Lipson KE, Tomai MA, Larson CJ, Vasilakos JP. TLR7 agonist 852A inhibition of tumor cell proliferation is dependent on plasmacytoid dendritic cells and type I IFN. J Interferon Cytokine Res. 2008 Apr;28(4):253-63.