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编 号:F756864
分子式:C22H21ClN2O5S
分子量:460.93
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生物活性:
GPX4-IN-4 (Compound 24) is a potent GPX4 inhibitor. GPX4-IN-4 can be used for the research of cancer.

体内研究:
GPX4-IN-4 (Compound 24; 100 and 200 mg/kg; i.p.; once) 在小鼠中作用于肾脏的 GPX4 并引发 PD 标志物的表达。尽管在肿瘤组织块中观察到部分目标结合,但 GPX4-IN-4 (50 mg/kg; i.p.; daily for 20 days) 对小鼠 WSU-DLCL2 肿瘤生长没有影响。Animal Model:SCID/Beige mice
Dosage:100 and 200 mg/kg
Administration:IP, once
Result:The GPX4 band was shifted. Engaged kidney GPX4 and induced PD markers.
Animal Model:SCID/Beige mice
Dosage:30 and 100 mg/kg
Administration:IP (Pharmacokinetic Analysis)
Result:PK Properties of GPX4-IN-4 (Compound 24)Doset1/2 (h) Cmax (μg/mL) AUC (μg*h/mL)
30 (IP)0.50.92 (±0.24)1.89 (±0.17)
100 (IP)1.75.31 (±0.53)16.20 (±1.70)


体外研究:
GPX4-IN-4 (Compound 24; 0-1000 nM; 0-24 h) inhibits HT1080 cell viability in a concentration- and time- dependent manner.GPX4-IN-4 (0-10 μM; 72 h) inhibits NCI-H1703 cell viability with EC50s of 0.117 μM and 4.74 μM without and with Fer-1 (HY-100579), respectively.
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