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Purity: ≥98%
RSL3 is a novel and potent inhibitor of glutathione peroxidase 4 (GPX4), which is able to reduce the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
ln Vitro |
With an IC50 of 5.8 μM in HN3-rslR cells and 0.48 μM in HN3 cells, RSL3 (0-8 μM, 72 hours) significantly lowers the viability of HN3 cells [1]. In HN3-rslR cells, RSL3 (0-8 μM, 24 hours) inactivates Keap1, raises the expression of p62 and Nrf2, and decreases the expression of GPX4 protein [1].
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ln Vivo |
Factor HN3R cell tumor growth can be markedly inhibited by combining trigonelline with RSL3 (100 mg/kg, intratumoral injection, twice weekly for 20 days) [1].
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Cell Assay |
Cell viability assay[1]
Cell Types: HN3 cells, HN3-rslR Cell Tested Concentrations: 0-8 μM Incubation Duration: 72 hrs (hours) Experimental Results: IC50 values in HN3 and HN3-rslR cells were 0.48 µM and 5.8 µM respectively[1] . Western Blot Analysis [1] Cell Types: HN3-rslR Cell Tested Concentrations: 0-8 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited GPX4 expression, increased p62 and Nrf2 levels, and diminished Keap1 levels. |
Animal Protocol |
Animal/Disease Models: Tenweeks old athymic BALB/c male nude mice (nu/nu) carrying HN3R cells [1]
Doses: 100 mg/kg combined with trigonelline (50 mg/kg): intratumoral injection, Experimental Results: Significant reduction in tumor volume in mice treated with trigonelline twice a week for 20 days. |
References |
[1]. Shin D, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.
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Molecular Formula |
C23H21CLN2O5
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Molecular Weight |
440.8762
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CAS # |
1219810-16-8
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SMILES |
ClCC(N1[C@@H](C(=O)OC)CC2C3=CC=CC=C3NC=2[C@@H]1C1C=CC(C(=O)OC)=CC=1)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~226.82 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (11.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.56 mg/mL (1.27 mM) (saturation unknown) in 10% DMF 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 5: 20 mg/mL (45.36 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2682 mL | 11.3410 mL | 22.6819 mL | |
5 mM | 0.4536 mL | 2.2682 mL | 4.5364 mL | |
10 mM | 0.2268 mL | 1.1341 mL | 2.2682 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.