Darbufelone 是 PGF2α 和 LTB4 的非竞争性双重抑制剂。 Dabfilon 有效抑制 PGHS-2，对 PGHS-2 和 PGHS-1 的 Ki 为 10 μM，IC50 为 0.19 μM 和 20 μM。
产品描述
Darbufelone is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.
体外活性
Darbufelone (5 - 60 μM) increases the cell growth inhibitory effects in A549, H520 and H460 cell lines with IC50s of 20, 21 and 15 μM[2].
体内活性
Darbufelone (80 mg/kg/day) decreases the tumor volumes in a time-dependent manner. Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, Darbufelone (80 mg/kg/day) reduces the tumor weight by 30.2%[2].
Cas No.
139226-28-1
分子式
C18H24N2O2S
分子量
332.46
别名
达布非酮;CI-1004
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
