FLI-06
(Synonyms: 1,4,5,6,7,8-六氢-2,7,7-三甲基-4-(4-硝基苯基)-5-氧代-3-喹啉羧酸环己基酯) 目录号 : GC10211
A Notch inhibitor
Cas No.:313967-18-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1]. |
References: [1]. Kramer A, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8. | |
FLI-06 is a novel inhibitor of Notch signaling with EC50 value of 2.3uM [1].
Notch signaling plays an important role in numerous cell-fate decisions, and its aberrant activity leads to cancer and developmental disorders [1].
Treatment of HeLa NotchΔE-eGFP cells with FLI-06 resulted in accumulation of NotchΔE-eGFP and reduced NICD-eGFP production. The phenotype was fully reversible within 1–4 h when washing out of FLI-06, which indicated that FLI-06 is not acutely toxic in cells [1]. In FLI-06 treated cells, Aβ secretion reduced significantly but not APPCTF accumulation, suggesting that FLI-06 acts upstream of α-secretase and β-secretase cleavage. Immunofluorescence analysis of HeLa cells revealed that FLI-06 caused a complete disruption of the Golgi, which can be caused by interfering with membrane trafficking in the early secretory pathway or by disassembly of the microtubules17. FLI-06 inhibited ER exit and also elicited the tubule-to-sheet phenotype, which are related to each other [1].
References:
[1]. Krämer A, Mentrup T, Kleizen B, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol, 2013, 9(11): 731-738.
| Cas No. | 313967-18-9 | SDF | |
| 别名 | 1,4,5,6,7,8-六氢-2,7,7-三甲基-4-(4-硝基苯基)-5-氧代-3-喹啉羧酸环己基酯 | ||
| 化学名 | cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,6,8-tetrahydroquinoline-3-carboxylate | ||
| Canonical SMILES | CC1=C(C(C2=C(N1)CC(CC2=O)(C)C)C3=CC=C(C=C3)[N+](=O)[O-])C(=O)OC4CCCCC4 | ||
| 分子式 | C25H30N2O5 | 分子量 | 438.52 |
| 溶解度 | ≥ 16.1mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2804 mL | 11.402 mL | 22.804 mL |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5608 mL |
| 10 mM | 0.228 mL | 1.1402 mL | 2.2804 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。