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BSP16

产品编号 T61455 CAS 2727249-47-8

BSP16 is a highly potent and orally active STING agonist, capable of selectively stimulating the interferon genes pathway. This compound, BSP16, holds great potential for cancer research [1].

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BSP16, CAS 2727249-47-8

规格	价格/CNY	货期
500 μg	￥ 2,660	35日内发货
1 mg	￥ 4,950	35日内发货
5 mg	￥ 17,300	35日内发货

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生物活性

化学信息

存储 & 溶解度

产品描述	BSP16 is a highly potent and orally active STING agonist, capable of selectively stimulating the interferon genes pathway. This compound, BSP16, holds great potential for cancer research [1].
体外活性	BSP16 (0.1-100 μM) can selectively stimulate the STING pathway in ISG-THP1 and ISGRAW264.7 cells with EC 50 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]. 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.
体内活性	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. C max (μg/mL) AUG 0-∞ (h*μg/mL) t 1/2 (h) V ss (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
分子式	C16H18O5Se
CAS No.	2727249-47-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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