E3 ligase Ligand 2
(Synonyms: 2-(2,6-二氧代-哌啶-3-基)-4-羟基-异吲哚-1,3-二酮,Cereblon ligand 2; E3 ligase Ligand 2) 目录号 : GC32848
An active metabolite of thalidomide and a PROTAC synthetic intermediate
Cas No.:5054-59-1
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
E3 ligase ligand 2 is an active metabolite of thalidomide and an intermediate in the synthesis of proteolysis-targeting chimeras (PROTACs) containing thalidomide, a ligand for the E3 ubiquitin ligase cereblon (CRBN), used in targeted protein degradation.1,2 E3 ligase ligand 2 is formed from thalidomide via hydroxylation. It decreases the production of TNF-α induced by 12-O-tetradecanoylphorbol 13-acetate in THP-1 cells when used at a concentration of 30 ?M.3 E3 ligase ligand 2 (333 ?M) completely inhibits the proliferation of human umbilical vein endothelial cells (HUVECs). It inhibits VEGF- and FGF2-induced angiogenesis by 14% in a chicken chorioallantoic membrane (CAM) assay in utero when administered at a dose of 100 ?g/embryo.1
1.Marks, M.G., Shi, J., Fry, M.O., et al.Effects of putative hydroxylated thalidomide metabolites on blood vessel density in the chorioallantoic membrane (CAM) assay and on tumor and endothelial cell proliferationBiol. Pharm. Bull.25(5)597-604(2002) 2.Robb, C.M., Contreras, J.I., Kour, S., et al.Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)Chem. Commun. (Camb.)53(54)7577-7580(2017) 3.Nakamura, T., Noguchi, T., Kobayashi, H., et al.Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activityChem. Pharm. Bull. (Tokyo)54(12)1709-1714(2006)
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6466 mL | 18.2329 mL | 36.4657 mL |
| 5 mM | 0.7293 mL | 3.6466 mL | 7.2931 mL |
| 10 mM | 0.3647 mL | 1.8233 mL | 3.6466 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。