SCR7|1533426-72-0|-陌孚医药/Medlife

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SCR7

目录号: PC10325 纯度: ≥98%

CAS No. :1533426-72-0

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中文名称

SCR7

中文别名

2,3-二氢-5,6-二[(E)-(苯基亚甲基)氨基]-2-硫代-4(1H)-嘧啶酮;SCR7 抑制剂

英文名称

SCR7

英文别名

SCR7;SCR-7;SCR7 Discontinued;5,6-Bis((E)-benzylideneamino)-2-mercaptopyrimidin-4(3H)-one;BC600700;X3557;5,6-bis((E)-benzylideneamino)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one;7-Benzyl-4-(2-methylbenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one;5-(Benzylideneamino)-6-[(E)-benzylideneamino]-2-sulfanylidene-1H-pyrimidin-4-one

Cas No.

1533426-72-0

分子式

C₁₈H₁₄N₄Os

分子量

334.40

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.

性状

Solid

IC50 & Target[1][2]

DNA Ligase IV

CRISPR/Cas9

体外研究(In Vitro)

SCR7 (SCR7 pyrazine; 20-100 μM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs).
SCR7 (SCR7 pyrazine) treatment shows a dose-dependent decrease in cell proliferation with IC₅₀ values of 40 μM, 34 μM, 44 μM, 8.5 μM, 120 μM, 10 μM and 50 μM for MCF7, A549, HeLa, T47D, A2780, HT1080 and Nalm6 cells, respectively.
In MCF7 cells, SCR7 (SCR7 pyrazine; 20, 40 μM) treatment increases phosphorylation of ATM and activates p53, decreases MDM2, BCL2, resulting in activation of proapoptotic proteins, PUMA and BAX. And the shorter fragments of MCL1, PARP1, Caspase 3, and Caspase 9 cleavage are upregulated in a dose-dependent manner.

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

Western Blot Analysis

Cell Line:	MCF7 cells
Concentration:	20 μM, 40 μM, 100 μM
Incubation Time:	24 hours
Result:	Showed an increase in levels of gH2AX foci and protein.

体内研究(In Vivo)

SCR7 (SCR7 pyrazine; 10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan.

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

Animal Model:	BALB/c mice injected with breast adenocarcinoma cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; on alternate days (0, 2, 4, 6, 8, and 10)
Result:	Significantly reduced breast adenocarcinoma-induced tumor and increased lifespan.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Srivastava M, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. Cell. 2012 Dec 21;151(7):1474-87. [Information]

[2]. Lin C, et al. Increasing the Efficiency of CRISPR/Cas9-mediated Precise Genome Editing of HSV-1 Virus in Human Cells. Sci Rep. 2016 Oct 7;6:34531. [Information]

[3]. Supriya V Vartak, et al. Autocyclized and Oxidized Forms of SCR7 Induce Cancer Cell Death by Inhibiting Nonhomologous DNA End Joining in a Ligase IV Dependent Manner. FEBS J. 2018 Nov;285(21):3959-3976. [Information]

溶解度数据

体外研究:

DMSO : ≥ 45 mg/mL (134.57 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9905 mL	14.9526 mL	29.9052 mL
5 mM	0.5981 mL	2.9905 mL	5.9810 mL
10 mM	0.2991 mL	1.4953 mL	2.9905 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.48 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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 ddH?O 中，得到澄清透明的生理盐水溶液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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