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Synonyms:
GPX4 degrader-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | GPX4 degrader-1 (Compound RS-1) is a GPX4 degrader utilizing hydrophobic tag (HyT) technology, demonstrating a DC50 of 8.9 nM in HT1080 cells. It induces GPX4 degradation, triggers ferroptosis, and increases lipid ROS levels. In a mouse breast cancer model, GPX4 degrader-1 exhibits potent antitumor activity. |
| Targets & IC50 | GPX4:8.9 nM (DC50) |
| In vitro | GPX4 degrader-1 induces dose- and time-dependent, proteasome-mediated degradation of GPX4 in HT1080 fibrosarcoma cells, with a DC50 of 8.9 nM, when used at concentrations of 0.3-300 nM for 2-48 hours. After 48 hours of treatment, GPX4 degrader-1 promotes ferroptosis-mediated antiproliferative activity in cancer cell lines HT1080, A549, and 4T1, with IC50 values of 130 nM, 6.4 μM, and 700 nM, respectively. Additionally, GPX4 degrader-1, at concentrations of 0.5-2.0 μM for 24-48 hours, increases lipid ROS and MDA levels in HT1080 fibrosarcoma cells. |
| In vivo | In a 4T1 mouse breast cancer model, GPX4 degrader-1 (16-66 μmol/kg; intraperitoneal injection; once daily; [10 days]) effectively inhibits tumor growth in a dose-dependent manner. |
| Molecular Weight | 634.16 |
| Formula | C38H36ClN3O4 |
| Cas No. | 3057531-85-5 |
| Smiles | C(CCl)(=O)N1[C@H](C2=C(C=3C(N2)=CC=CC3)C[C@@H]1C(OC)=O)C4=CC=C(C(NCCCC(C5=CC=CC=C5)C6=CC=CC=C6)=O)C=C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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