INH154
目录号 : GC34150
INH154 is a potent inhibitor of Nek2 and Hec1 binding. NH154 binds to Hec1, thus blocking Hec1 phosphorylation by NEK2, and kills cancer cells at the nanomolar range.
Cas No.:1587705-63-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[1]Human triple negative breast cancer MDA-MB-468 cells, which expressed high levels of both Hec1 and Nek2, are used to test the efficacy of tumor growth in mouse xenograft. While tumor volumes reach ~100mm3, mice are randomly divided into 5 treatment groups and began to receive thrice-weekly intraperitoneal (i.p.) injections of vehicle control, 10 mg/kg INH41, 50 mg/kg INH41, 5 mg/kg INH154 or 20 mg/kg INH154. Treatment is continued for 6.5 weeks and the tumor sizes were measured[1]. |
References: [1]. Hu CM, et al. Novel small molecules disrupting Hec1/Nek2 interaction ablate tumor progression by triggering Nek2 degradation through a death-trap mechanism. Oncogene. 2015 Mar 5;34(10):1220-30. | |
INH154 is a potent inhibitor of Nek2 and Hec1 binding. NH154 binds to Hec1, thus blocking Hec1 phosphorylation by NEK2, and kills cancer cells at the nanomolar range.
[1] Yanfen Fang, Xiongwen Zhang. Cell Cycle. 2016;15(7):895-907.
| Cas No. | 1587705-63-2 | SDF | |
| Canonical SMILES | O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(N4CCCCC4)C=C3C)=CS2 | ||
| 分子式 | C22H24N4OS | 分子量 | 392.52 |
| 溶解度 | DMSO : 62.5 mg/mL (159.23 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 2.5476 mL | 12.7382 mL | 25.4764 mL |
| 5 mM | 0.5095 mL | 2.5476 mL | 5.0953 mL |
| 10 mM | 0.2548 mL | 1.2738 mL | 2.5476 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。