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编 号:F762432
分子式:C29H28O8S2
分子量:568.66
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1mg
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5mg
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生物活性:
MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide.

体内研究:
MSA-2 dimer (60 mg/kg;口服;50 天) 抑制肿瘤生长,并延长总生存期。 MSA-2 dimer (40 mg/kg;皮下注射;25天) 诱导肿瘤完全消退。MSA-2 dimer (60 mg/kg;口服;4 小时) 增加肿瘤中的促炎细胞因子 (IFN-β) 水平。 在肿瘤中观察到的 MSA-2 dimer (60 mg/kg;sc;4 小时) 浓度高于血浆或其他非肿瘤组织。 MSA-2 dimer (THP-1 细胞) 诱导 TBK1 和 IR 的磷酸化。MSA-2 dimer (10 μM 和 33 μM;巨噬细胞) 诱导 IFN-β。Animal Model:B16F10 tumor-bearing mice
Dosage:60 mg/kg
Administration:P.o.; 50 days
Result:Inhibited tumor growth and prolonged overall survival.
Animal Model:C57BL6 mice
Dosage:40 mg/kg
Administration:S.c.; 25 days
Result:Induced complete tumor regression.
Animal Model:C57BL6 mice
Dosage:60 mg/kg
Administration:P.o.; 4 hours
Result:Increased proinflammatory cytokine (IFN-β) level in tumors.
Animal Model:C57BL6 mice
Dosage:50 mg/kg
Administration:S.c.; 4 hours
Result:MSA-2 concentrations were observed in tumors than in plasma or other nontumor tissues.
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