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编 号：F755003
分子式：C16H18O5Se
分子量：369.27
分子式：C16H18O5Se
分子量：369.27
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CAS No: 2727249-47-8
产品详情
生物活性：
BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
体内研究：
BSP16 (po, 50 mg/kg; iv, 5 mg/kg) has well lerated and excellent pharmacokinetic profile.BSP16 (oral, 15 and 30 mg/kg, q3d; oral, 20 mg/kg, q5d) induces tumor regression and durable antitumor immunity.Animal Model:MC38 (colon carcinoma) syngeneic tumor model
Dosage:15, 30 mg/kg
Administration:oral, q3d
Result:Exhibited tolerated and excellent antitumor efficacy, experienced complete tumor regression (CR) after day 21.Resulted in robust induction of IFNB and IL6 (30 mg/kg).
Animal Model:CT26 (colon carcinoma) tumor model
Dosage:20 mg/kg
Administration:oral, q5d
Result:Exhibited tolerated and induced tumor regression in all treated mice within 30 days.Led to a substantial elevation of IFNB in the plasma in CT26 bearing mice.
Animal Model:Rats
Dosage:5 mg/kg, 50 mg/kg
Administration:oral and i.v
Result:compd.adm.Cmax(μg/mL)AUG0-∞(h*μg/mL)t1/2(h)Vss(L/kg)CL(L/h/kg)F(%)
BSP16 po(50 mg/kg)58.2315.91.600.380.16107
iv(5 mg/kg) 29.41.040.260.17
体外研究：
BSP16 (0.1-100 μM) can selectively stimulate the STING pathway in ISG-THP1 and ISGRAW264.7 cells with EC50 values of 9.24 and 5.71 μM, respectively.BSP16 (10, 25, 50 μM; 1, 3, 6 h) strongly activates STING signaling in human and mouse cells and binds STING as a homodimer.BSP16 exhibits a promising absorption, distribution, metabolism, excretion and toxicity.
BSP16 is a potent, orally active stimulator of interferon genes (STING) agonist. BSP16 can selectively stimulate the STING pathway. BSP16 can be used for the research of cancer.
体内研究：
BSP16 (po, 50 mg/kg; iv, 5 mg/kg) has well lerated and excellent pharmacokinetic profile.BSP16 (oral, 15 and 30 mg/kg, q3d; oral, 20 mg/kg, q5d) induces tumor regression and durable antitumor immunity.Animal Model:MC38 (colon carcinoma) syngeneic tumor model
Dosage:15, 30 mg/kg
Administration:oral, q3d
Result:Exhibited tolerated and excellent antitumor efficacy, experienced complete tumor regression (CR) after day 21.Resulted in robust induction of IFNB and IL6 (30 mg/kg).
Animal Model:CT26 (colon carcinoma) tumor model
Dosage:20 mg/kg
Administration:oral, q5d
Result:Exhibited tolerated and induced tumor regression in all treated mice within 30 days.Led to a substantial elevation of IFNB in the plasma in CT26 bearing mice.
Animal Model:Rats
Dosage:5 mg/kg, 50 mg/kg
Administration:oral and i.v
Result:compd.adm.Cmax(μg/mL)AUG0-∞(h*μg/mL)t1/2(h)Vss(L/kg)CL(L/h/kg)F(%)
BSP16 po(50 mg/kg)58.2315.91.600.380.16107
iv(5 mg/kg) 29.41.040.260.17
体外研究：
BSP16 (0.1-100 μM) can selectively stimulate the STING pathway in ISG-THP1 and ISGRAW264.7 cells with EC50 values of 9.24 and 5.71 μM, respectively.BSP16 (10, 25, 50 μM; 1, 3, 6 h) strongly activates STING signaling in human and mouse cells and binds STING as a homodimer.BSP16 exhibits a promising absorption, distribution, metabolism, excretion and toxicity.
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