diABZI STING agonist-1 trihydrochloride
目录号 : KM6709 CAS No. : 2138299-34-8 纯度 : 98%

diABZI STING agonist-1 (trihydrochloride) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂,其在人和小鼠中的 EC50 值分分别为 130 nM 和 186 nM。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock

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生物活性

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

体外研究

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested.

体内研究

diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.
diABZI STING agonist-1 trihydrochloride (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/ml).
diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43.

Animal Model: Wild and Sting C57Blk6 mice
Dosage: 2.5 mg/kg
Administration: Subcutaneous injection; 2.5 mg/kg
Result: Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting mice.
Animal Model: Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice
Dosage: 3 mg/kg
Administration: Intravenous injection; 3 mg/kg
Result: Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC50 for mouse STING (200 ng/ml).
Animal Model: Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice
Dosage: 1.5 mg/kg
Administration: Intravenous injection; 1.5 mg/kg; 43 days
Result: Resulted in significant tumour growth inhibition and improved survival.
分子式
C42H54Cl3N13O7
分子量
959.32
CAS号
2138299-34-8
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (130.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0424 mL 5.2120 mL 10.4241 mL
5 mM 0.2085 mL 1.0424 mL 2.0848 mL
10 mM 0.1042 mL 0.5212 mL 1.0424 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.17 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
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