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[CAS NO. 2761004-85-5] GPX4-IN-3
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-141809 |
| Brand: | MCE |
| CAS: | 2761004-85-5 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 530.04 |
| Molecular Formula | C29H24ClN3O3S |
| SMILES | O=C(C(C1=CSC2=CC=CC=C21)N(C3=CC=C(C=C3)C4=CN=CO4)C(CCl)=O)NCCC5=CC=CC=C5 |
Summary
GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM [1] .
In Vitro
GPX4-IN-3 (26a) exhibits IC
50
values of 0.78 μM, 6.9 μM, 0.15 μM and 4.73 μM in 4T1, MCF-7, HT1080 and HT1080 (with Fer-1) cells, respectively
[1]
.
GPX4-IN-3 (26a) exhibits outstanding GPX4 inhibitory activity with a percent inhibition up to 71.7% at 1.0 μM compared to 45.9% of RSL-3
[1]
.
GPX4-IN-3 (26a) could significantly induce lipid peroxide (LPO) increase and effectively induce ferroptosis with satisfactory selectivity
[1]
.
GPX4-IN-3 (26a) is more likely to induce ferroptosis through the accumulation of intracellular peroxides via inhibiting GPX4 activity
[1]
.
GPX4-IN-3 (26a) significantly increased the level of ROS in 4T1 cells, which could also be reversed by Ferrostatin-1 (fer-1)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GPX4-IN-3 (26a) exertes antitumor activity and good biological safety in vivo
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Mouse 4T1 xenograft model [1] . |
| Dosage: | 15 and 30 mg/kg. |
| Administration: | Intravenous injection, every two days for a total of five times. |
| Result: | Significantly suppress tumor growth with a tumor growth inhibition (TGI) value of 33.2 and 55.1% at 15 and 30 mg/kg, respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 67.5 mg/mL ( 127.35 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8867 mL | 9.4333 mL | 18.8665 mL |
| 5 mM | 0.3773 mL | 1.8867 mL | 3.7733 mL |
| 10 mM | 0.1887 mL | 0.9433 mL | 1.8867 mL |
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