| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
GPX4-IN-1 (compound 28) (0.0005-10 mM; 24 hours) showed antiproliferative activity against 786-O, SJSA-1 and A431 cells, with IC50 values of 0.004, 0.016 and 2.9 µM, respectively [1].
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|---|---|
| ln Vivo |
GPX4-IN-1 (5 mg/kg in mice and 2 mg/kg in rats; intravenous injection) showed favorable pharmacokinetic characteristics in mice and rats [1].
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| Animal Protocol |
Animal/Disease Models: Male Balb/c mice, 6-8 weeks old, 22-25 g; Male SD rats, 6-8 weeks old, 200-250 g [1]
Doses: 5 mg/kg for mice, 2 mg/kg for rats. Route of Administration: Intravenous injection. Experimental Results: The mice showed good pharmacokinetic characteristics. The half-life (T1/2) in mice was 3.5 hours, the maximum concentration (Cmax) was 5446 ng/mL, the average concentration (AUC) was 1635 ng·h/mL, the minimum concentration (CL) was 49 mL/min/kg, and the maximum volume (Vd) was 14.7 L/kg. The half-life (T1/2) in rats was 3.15 hours, the maximum concentration (Cmax) was 3529 ng/mL, the average concentration (AUC) was 1082 ng·h/mL, and the CL was 30 mL/min/kg. The Vd in rats was 8.2 L/kg. |
| References |
| Molecular Formula |
C33H40N2O2
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|---|---|
| Molecular Weight |
496.68
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| CAS # |
2375356-92-4
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| Related CAS # |
GPX4-IN-2
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| Appearance |
White to off-white solid
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| SMILES |
COC1=CC=C2C(C[C@H](CCCC)N([C@H]2C3=CC=C(NC4(C[C@H](C5)C6)C[C@H]6C[C@H]5C4)C=C3)C(C#C)=O)=C1
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| HS Tariff Code |
2934.99.9001
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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 (~201.34 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (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 canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.03 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0134 mL | 10.0668 mL | 20.1337 mL | |
| 5 mM | 0.4027 mL | 2.0134 mL | 4.0267 mL | |
| 10 mM | 0.2013 mL | 1.0067 mL | 2.0134 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.
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