GNE-987 GSH linker-2
Based on 1 Customer Validation
GNE-987 GSH linker-2 is a drug-linker conjugates for ADC. GNE-987 GSH linker-2 is a conjugation of PROTAC GNE-987 (HY-129937A) and ADC linker GSH linker-2 (HY-182740), and can be used to prepare antibody-drug conjugates (ADC) for BRD4 degradation. GNE-987 GSH linker-2 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 99.48%
- Formula: C61H75F2N9O12S4
- Molecular Weight:1292.56
-
Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
BRD4 |
GNE-987 GSH linker-2 (Compound 9a) can be used for the synthesis of ADC STEAP1-9a-D2 potently degrades BRD4 with a DC50 of 0.23 nM and inhibits PC3-S1 cell proliferation with an IC50 of 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Appearance Solid
-
Molecular Weight 1292.56
-
Formula C61H75F2N9O12S4
-
Color Off-white to light yellow
-
SMILES
CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCCCCCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O)OC(OC[C@@H](C)SS(C)(=O)=O)=O)=O)C=C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (77.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (273 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.7737 mL | 3.8683 mL | 7.7366 mL | 19.3415 mL |
| 5 mM | 0.1547 mL | 0.7737 mL | 1.5473 mL | 3.8683 mL | |
| 10 mM | 0.0774 mL | 0.3868 mL | 0.7737 mL | 1.9341 mL | |
| 15 mM | 0.0516 mL | 0.2579 mL | 0.5158 mL | 1.2894 mL | |
| 20 mM | 0.0387 mL | 0.1934 mL | 0.3868 mL | 0.9671 mL | |
| 25 mM | 0.0309 mL | 0.1547 mL | 0.3095 mL | 0.7737 mL | |
| 30 mM | 0.0258 mL | 0.1289 mL | 0.2579 mL | 0.6447 mL | |
| 40 mM | 0.0193 mL | 0.0967 mL | 0.1934 mL | 0.4835 mL | |
| 50 mM | 0.0155 mL | 0.0774 mL | 0.1547 mL | 0.3868 mL | |
| 60 mM | 0.0129 mL | 0.0645 mL | 0.1289 mL | 0.3224 mL |
Powered by Bioz