E3 ligase Ligand 1 |
| カタログ番号GC32711 |
E3 リガーゼ リガンド 1 (VHL リガンド 2 塩酸塩) は、(S,R,S)-AHPC ベースの VHL リガンドであり、フォン ヒッペル-リンダウ (VHL) タンパク質の動員に使用されます。 E3 リガーゼ リガンド 1 は、フォン ヒッペル-ランダウ (VHL) E3 リガーゼ ベースの BET PROTAC デグレーダーである ARV-771 の合成に使用できます。 ARV-771 は、去勢抵抗性前立腺癌 (CRPC) 細胞の BET タンパク質を DC50 <1 nM で強力に分解します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1948273-03-7
Sample solution is provided at 25 µL, 10mM.
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E3 ligase Ligand 1 is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.
E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand[1]. E3 ligase Ligand 1 is used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].
[1]. WO/2017/030814A1 [2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129
| Cas No. | 1948273-03-7 | SDF | |
| Canonical SMILES | N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O.Cl | ||
| Formula | C23H33ClN4O3S | M.Wt | 481.05 |
| 溶解度 | DMSO : ≥ 63 mg/mL (130.96 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0788 mL | 10.3939 mL | 20.7879 mL |
| 5 mM | 0.4158 mL | 2.0788 mL | 4.1576 mL |
| 10 mM | 0.2079 mL | 1.0394 mL | 2.0788 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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