SCR7 pyrazine
(Synonyms: SCR7 吡嗪) 目录号 : GC14335SCR7 pyrazine 是一种 DNA 连接酶 IV 抑制剂,以连接酶 IV 依赖性方式阻断非同源末端连接 (NHEJ)。 SCR7 吡嗪也是一种 CRISPR/Cas9 增强剂,可提高 Cas9 介导的同源定向修复 (HDR) 的效率。 SCR7 pyrazine 可诱导细胞凋亡并具有抗癌活性。
Cas No.:14892-97-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SCR7 pyrazine is an inhibitor of DNA ligase IV [1].
DNA Ligase IV is involved in sealing of double-strand breaks (DSBs) during nonhomologous end-joining (NHEJ). DSBs have been considered as one of the most lethal types of DNA damage within cells. Unrepaired DSBs may lead to chromosomal rearrangements such as translocations and deletions, resulting in oncogenic transformations or cell death. In higher eukaryotes, NHEJ is one of the primary mechanisms of DSB repair and is active throughout the cell cycle. NHEJ plays a major role in providing resistance to cancer cells to these radio- and chemotherapy agents [1].
SCR7 blocked Ligase IV-mediated joining by interfering with its DNA binding in cell-free repair system. SCR7 inhibited NHEJ in a Ligase IV-dependent manner within cells, and activated the intrinsic apoptotic pathway. SCR7 dose-dependent decreased cell proliferation in MCF7, A549, and HeLa cells with an IC50 of 40, 34, and 44 μM, respectively. In T47D, A2780, and HT1080 cells, the IC50 values were 8.5, 120, and 10 μM, respectively [1].
SCR7 treatment (10 mg/kg, six doses) significantly reduced breast adenocarcinoma-induced tumor and impeded tumor progression in mouse models in mouse models. Coadministered of SCR7 with DSB-inducing therapeutic modalities significantly enhanced their sensitivity.
Reference:
[1] Srivastava M, Nambiar M, Sharma S, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression[J]. Cell, 2012, 151(7): 1474-1487.
Cas No. | 14892-97-8 | SDF | |
别名 | SCR7 吡嗪 | ||
化学名 | 2,3-dihydro-6,7-diphenyl-2-thioxo-4(1H)-pteridinone | ||
Canonical SMILES | O=C(C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)NC1=N4)NC4=S | ||
分子式 | C18H12N4OS | 分子量 | 332.4 |
溶解度 | ≥ 33.2mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0084 mL | 15.0421 mL | 30.0842 mL |
5 mM | 0.6017 mL | 3.0084 mL | 6.0168 mL |
10 mM | 0.3008 mL | 1.5042 mL | 3.0084 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。