360A
(Synonyms: 3,3'-[2,6-吡啶二基二(羰基亚氨基)]二[1-甲基喹啉鎓],360 A) 目录号 : GC15389
360A 是 G-quadruplex 的选择性稳定剂，也抑制端粒酶活性，在 TRAP-G4 试验中对端粒酶的 IC50 为 300 nM。
Cas No.:794458-56-3
Sample solution is provided at 25 µL, 10mM.
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Description: IC50 Value: N/A 360A is a 2,6-pyridine-dicarboxamide derivative displaying strong affinity and selectivity for G-quadruplex structures and selective telomerase inhibition in vitro assays. 360A is a G-quadruplex ligand, which can influence the consequence of G-quadruplex formation and/or stabilization. in vitro: We found a S-phase accumulation in ATM-proficient, but not in ATM-deficient EBV-lymphocytes treated with 360A before induction of cell death. However, ATM status did not modify cell cycle distribution in 360A-treated SV40-fibroblasts and HeLa cells compared to DMSO treated controls [1]. DNA-PKcs-dependent NHEJ was responsible for sister telomere fusions as a direct consequence of G-quadruplex formation and/or stabilization induced by 360A on parental telomere G strands. NHEJ and HR activation at telomeres altered mitotic progression in treated cells [2]. This compound was shown to display a potent affinity and selectivity for telomeric G-quadruplex DNA over duplex DNA and to induce delayed growth inhibition in HT1080 tumor cell line [3]. in vivo: N/A Clinical trial: N/A
Cell experiment: | The cell proliferation reagent WST-1 assay is performed. In brief, cells are seeded at various densities, depending on cell type (0.25-4 × 103 cells/well in 100 μL complete medium), in 96-well culture plates and treated with various concentrations (0.1-20 μM) of 360A or the corresponding concentrations of DMSO (control wells) for 3 or 7 days at 37°C in an atmosphere containing 5% CO2. For 7-day assays, the medium is changed on day 3. Experiments are performed in triplicate[1]. |
References: [1]. Pennarun G, et al. Apoptosis related to telomere instability and cell cycle alterations in human glioma cells treated by new highly selective G-quadruplex ligands. Oncogene. 2005 Apr 21;24(18):2917-28. | |
| Cas No. | 794458-56-3 | SDF | |
| 别名 | 3,3'-[2,6-吡啶二基二(羰基亚氨基)]二[1-甲基喹啉鎓],360 A | ||
| 化学名 | 3,3'-((pyridine-2,6-dicarbonyl)bis(azanediyl))bis(1-methylquinolin-1-ium) | ||
| Canonical SMILES | CN1=C2C=CC=CC2=C/C(C=1)=[NH+]/C(C3=NC(C(/[NH+]=C4C=C5C=CC=CC5=N(C)=C/4)=O)=CC=C3)=O | ||
| 分子式 | C27H23N5O2 2+ | 分子量 | 449.5 |
| 溶解度 | Soluble 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2247 mL | 11.1235 mL | 22.2469 mL |
| 5 mM | 0.4449 mL | 2.2247 mL | 4.4494 mL |
| 10 mM | 0.2225 mL | 1.1123 mL | 2.2247 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet