BSP16 是一种有效的干扰素基因激动剂 (STING) 激动剂，具有口服活性。 BSP16 可以选择性地刺激 STING 通路。BSP16 可用于癌症研究。
| 生物活性 | BSP16 is a potent, orally activestimulator of interferon genes (STING)agonist. BSP16 can selectively stimulate theSTINGpathway. BSP16 can be used for the research ofcancer[1]. |
| IC50& Target | IC50 for STING: 9.24 μM (ISG-THP1 cells); 5.71 μM (ISGRAW264.7 cells)[1] |
体外研究
(In Vitro) | BSP16 (0.1-100 μM) can selectively stimulate the STING pathway in ISG-THP1 and ISGRAW264.7 cells with EC50values of 9.24 and 5.71 μM, respectively[1].
BSP16 (10, 25, 50 μM; 1, 3, 6 h) strongly activates STING signaling in human and mouse cells and binds STING as a homodimer[1].
BSP16 exhibits a promising absorption, distribution, metabolism, excretion and toxicity[1].
RT-PCR[1] | Cell Line: | ISG-THP1 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 1, 3, 6 h | | Result: | Robustly induced mRNA expression of target genes IFNβ, CXCL10, and IL6 in response to STING activation, in a time and concentration-dependent manner in ISGTHP1 cells. |
Western Blot Analysis[1] | Cell Line: | ISG-THP1 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 1, 3, 6 h | | Result: | Rapidly increased the phosphorylation of TBK1 and IRF3 in a concentration-dependent manner. |
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体内研究
(In Vivo) | BSP16 (po, 50 mg/kg; iv, 5 mg/kg) has well lerated and excellent pharmacokinetic profile[1].
BSP16 (oral, 15 and 30 mg/kg, q3d; oral, 20 mg/kg, q5d) induces tumor regression and durable antitumor immunity[1].
| Animal Model: | MC38 (colon carcinoma) syngeneic tumor model[1] | | 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[1] | | 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[1] | | 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) | 58.2 | 315.9 | 1.60 | 0.38 | 0.16 | 107 | | iv(5 mg/kg) | | 29.4 | 1.04 | 0.26 | 0.17 | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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