1. Immunology/Inflammation
  2. STING
  3. BSP16

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。

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BSP16 Chemical Structure

BSP16 Chemical Structure

CAS No. : 2727249-47-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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 EC50 values 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
分子量

369.27

Formula

C16H18O5Se

CAS 号
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.

纯度 & 产品资料
参考文献

BSP16 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BSP16
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HY-151264
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