耗材描述
Trilexium
产品活性:Trilexium (TRX-E-009-1) 是第三代苯并吡喃,结构与 TRX-E-002-1 (HY-114250) 相关。Trilexium 增加 p21 蛋白表达并诱导细胞凋亡 (apoptosis)。Trilexium 解聚微管。Trilexium 显示出广泛的抗癌活性。
产品来源: https://www.medchemexpress.cn/trilexium.html
研究领域:Cytoskeleton | Apoptosis | Epigenetics | Cell Cycle/DNA Damage
作用靶点:Microtubule/Tubulin | Apoptosis | PARP | Caspase
In Vitro: Trilexium shows activity against a broad range of cancer types. Of the 240 cell lines assessed in the Eurofin’s Oncopanel, 10 cell lines shows IC50 > 30 μM, of the remaining 230 cell lines, the average IC50 is 0.428 μM.
Trilexium (300 nM, 4 h) disrupts microtubule networks in Hela cells.
Trilexium (1-5 μM) leads to increased protein expression of p21, c-PARP, and c-Caspase 3 in HSJD-DIPG007 cells.
Trilexium (0-2 μM) restores H3K27 trimethylation and increases H3K27 acetylation in HSJD-DIPG007 cells.
In Vivo: Trilexium (5-60 mg/kg, IV daily for 15 days) significantly reduces tumour volume in vivo.
Trilexium (80 mg/kg, IV daily for 5 days) disrupts microtubules in vivo.
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