PROTAC GPX4 degrader-4
Based on 1 Customer Validation
PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)).
(Pink: GPX4 ligand (HY-N0193); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W013907)).
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 3071165-43-7
- Formula: C43H58N2O13
- Molecular Weight:810.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All PROTACs Isoforms
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Biological Activity
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GPX4 |
Cereblon |
Chemical Information
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CAS No. 3071165-43-7
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Appearance Solid
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Molecular Weight 810.93
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Formula C43H58N2O13
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Color White to off-white
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SMILES
C[C@@H]1[C@@]2([H])[C@]34[C@](O[C@](OO3)(CC[C@@]4([H])[C@@H](CC2)C)C)([H])O[C@H]1OC(CCC(OCCCCCCCCCCCOC5=C6C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)=CC=C5)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 101 mg/mL (124.55 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. 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. 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.52 mg/mL (3.11 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.52 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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
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Data Sheet (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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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. 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 |
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| DMSO | 1 mM | 1.2332 mL | 6.1658 mL | 12.3315 mL | 30.8288 mL |
| 5 mM | 0.2466 mL | 1.2332 mL | 2.4663 mL | 6.1658 mL | |
| 10 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0829 mL | |
| 15 mM | 0.0822 mL | 0.4111 mL | 0.8221 mL | 2.0553 mL | |
| 20 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 25 mM | 0.0493 mL | 0.2466 mL | 0.4933 mL | 1.2332 mL | |
| 30 mM | 0.0411 mL | 0.2055 mL | 0.4111 mL | 1.0276 mL | |
| 40 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL | |
| 50 mM | 0.0247 mL | 0.1233 mL | 0.2466 mL | 0.6166 mL | |
| 60 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5138 mL | |
| 80 mM | 0.0154 mL | 0.0771 mL | 0.1541 mL | 0.3854 mL | |
| 100 mM | 0.0123 mL | 0.0617 mL | 0.1233 mL | 0.3083 mL |