Bioactivity | 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]. |
Invitro | 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[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. 0 --> Trilexium 相关抗体: |
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: |
CAS | 1983180-82-0 |
Formula | C24H23FO6 |
Molar Mass | 426.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Stevenson AJ, et al. Mechanism of action of the third generation benzopyrans and evaluation of their broad anti-cancer activity in vitro and in vivo. Sci Rep. 2018 Mar 23;8(1):5144. [2]. Ehteda A, et al. Microtubule-Targeting Combined with HDAC Inhibition Is a Novel Therapeutic Strategy for Diffuse Intrinsic Pontine Gliomas. Mol Cancer Ther. 2023 Dec 1;22(12):1413-1421. |