产品
编 号:F602072
分子式:C20H20Cl2N4O4
分子量:451.3
产品类型
结构图
CAS No: 2421119-60-8
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产品详情
生物活性:
JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors.
体内研究:
JKE-1674 (50?mg/kg; p.o.) can be detected in the serum of mice dosed orally with the compound.Animal Model:SCID mice
Dosage:50?mg/kg (Pharmacokinetic Analysis)
Administration:P.o.
Result:Could be detected in the serum of mice dosed orally with the compound.
体外研究:
JKE-1674 exhibits activity indistinguishable from that of ML210 in cellular target engagement assays including yielding the same +434Da GPX4 adduct in cells. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML210 and is completely rescued by ferroptosis inhibitors. JKE-1674 forms a nitrile-oxide electrophile in cells. JKE-1674 dehydration yields a nitrile-oxide electrophile that binds GPX4. JKE-1674 exhibits far greater stability than chloroacetamide inhibitors.