1. Cytoskeleton Apoptosis Epigenetics Cell Cycle/DNA Damage
  2. Microtubule/Tubulin Apoptosis PARP Caspase
  3. Trilexium

Trilexium  (Synonyms: TRX-E-009-1)

目录号: HY-157800 纯度: 99.70%
COA 产品使用指南

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。

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Trilexium Chemical Structure

Trilexium Chemical Structure

CAS No. : 1983180-82-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity[1][2].

体外研究
(In Vitro)

Trilexium 显示出针对多种癌症类型的活性。 在 Eurofin 的 Oncopanel 中评估的 240 个细胞系中,有 10 个细胞系显示 IC50 > 30 μM,其余 230 个细胞系中,平均 IC50 为 0.428 μM< sup>[1]。
Trilexium (300 nM, 4 h) 会破坏 Hela 细胞中的微管网络[1]
Trilexium (1-5 μM) 会导致 HSJD-DIPG007 细胞中 p21、c-PARP 和 c-Caspase 3 的蛋白表达增加[2]
Trilexium (0-2 μM) 可恢复 HSJD-DIPG007 细胞中的 H3K27 三甲基化并增加 H3K27 乙酰化[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Trilexium (5-60 mg/kg,每天静脉注射,持续 15 天)可显著减少体内肿瘤体积[1]
Trilexium (80 mg/kg,每天静脉注射,持续 5 天)会破坏体内微管[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57/BL6 mice (n = 8 mice per group, subcutaneous mouse xenograft model of BRAF mutant (BRAFV600E) melanoma (A375))[1]
Dosage: 5 and 60 mg/kg
Administration: IV (tail vein injection), daily for 15 days
Result: Resulted in a tumour growth inhibition at 60 mg/kg. Significantly improved survival at 60 mg/kg.
Animal Model: A375 xenografts mice[1].
Dosage: 80 mg/kg
Administration: IV, daily for 5 days
Result: Resulted in a loss of the long microtubule filaments in favour of shorter filaments and dispersed tubulin staining.
分子量

426.43

Formula

C24H23FO6

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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