diABZI STING agonist-1

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CAS NO:

2138299-33-7

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

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

IC₅₀& Target

STING^[1].

体外研究
(In Vitro)

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^[1].

体内研究
(In Vivo)

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

Animal Model:	Wild and Sting^–/–C57Blk6 mice^[1]
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^[1]
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 EC₅₀for mouse STING (200 ng/ml).

Animal Model:	Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:	1.5 mg/kg
Administration:	Intravenous injection; 1.5 mg/kg; 43 days
Result:	Resulted in significant tumour growth inhibition and improved survival.

分子量

849.94

性状

Solid

Formula

C₄₂H₅₁N₁₃O₇

CAS 号

2138299-33-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 140 mg/mL(164.72 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。

*以上所有助溶剂都可在本网站选购。