For research use only. Not for therapeutic Use.
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].
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[1].
Trilexium (300 nM, 4 h) disrupts microtubule networks in Hela cells[1].
Trilexium (1-5 μM) leads to increased protein expression of p21, c-PARP, and c-Caspase 3 in HSJD-DIPG007 cells[2].
Trilexium (0-2 μM) restores H3K27 trimethylation and increases H3K27 acetylation in HSJD-DIPG007 cells[2].
Trilexium (5-60 mg/kg, IV daily for 15 days) significantly reduces tumour volume in vivo[1].
Trilexium (80 mg/kg, IV daily for 5 days) disrupts microtubules in vivo[1].
| Catalog Number | I040073 |
| CAS Number | 1983180-82-0 |
| Synonyms | (3R,4S)-4-(3-fluoro-4-hydroxyphenyl)-3-(4-hydroxy-3,5-dimethoxyphenyl)-8-methyl-3,4-dihydro-2H-chromen-7-ol |
| Molecular Formula | C24H23FO6 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H23FO6/c1-12-18(26)7-5-15-22(13-4-6-19(27)17(25)8-13)16(11-31-24(12)15)14-9-20(29-2)23(28)21(10-14)30-3/h4-10,16,22,26-28H,11H2,1-3H3/t16-,22-/m0/s1 |
| InChIKey | RDQGRFVVYZSNMO-AOMKIAJQSA-N |
| SMILES | CC1=C(C=CC2=C1OCC(C2C3=CC(=C(C=C3)O)F)C4=CC(=C(C(=C4)OC)O)OC)O |
| 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. |
