diABZI STING agonist-1|cas:2138299-33-7|西域试剂

diABZI STING agonist-1,99.12%

产品编号：Bellancom-112921A| CAS NO：2138299-33-7| 分子式：C₄₂H₅₁N₁₃O₇| 分子量：849.94

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-112921A		￥3500.00	杭州北京（现货）
Bellancom-112921A		￥5900.00	杭州北京（现货）

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diABZI STING agonist-1

产品介绍

diABZI STING agonist-1 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 值分别为 130 nM 和 186 nM。

生物活性

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.

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.

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

体内研究

diABZI STING agonist-1 (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo.
diABZI STING agonist-1 (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 (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.

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

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.

体内研究

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (117.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.1766 mL	5.8828 mL	11.7655 mL
5 mM	0.2353 mL	1.1766 mL	2.3531 mL
10 mM	0.1177 mL	0.5883 mL	1.1766 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 (sealed storage, away from moisture and light)。-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: ≥ 3.5 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 3.5 mg/mL (4.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 35.0 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3.5 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 3.5 mg/mL (4.12 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 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。