Trilexium
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 99.70%
- CAS No.: 1983180-82-0
- Formula: C24H23FO6
- Molecular Weight:426.43
-
Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-N0674
DehydrocorydalineAlkaloid -
HY-N4103
FucosterolBioactive Sterol -
HY-N1970
5,7-DihydroxychromoneNrf2/ARE Pathway Activator -
HY-108632
BYK204165PARP1 Inhibitor -
HY-128400
4'-MethoxychalconePARP Activator -
HY-N7661
4β-Hydroxywithanolide EAdipogenesis Inhibitor -
HY-75706
N-Descyclopropanecarbaldehyde OlaparibPARP Inhibitor -
HY-156432
ALK-IN-26ALK Inhibitor -
HY-N1970R
5,7-Dihydroxychromone (Standard)Analytical Standard -
HY-108632R
BYK204165 (Standard)Reference Standard -
HY-N4103R
Fucosterol (Standard) -
HY-128400R
4'-Methoxychalcone (Standard)PARP Activator
All Caspase Isoforms
More
Biological Activity
Description
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[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Trilexium (80 mg/kg, IV daily for 5 days) disrupts microtubules in vivo[1].
MedChemExpress (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.
Chemical Information
-
CAS No. 1983180-82-0
-
Appearance Solid
-
Molecular Weight 426.43
-
Formula C24H23FO6
-
Color White to off-white
-
SMILES
OC1=C(OC)C=C([C@H]2[C@@H](C3=CC(F)=C(C=C3)O)C4=CC=C(O)C(C)=C4OC2)C=C1OC
-
Synonyms
TRX-E-009-1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 300 mg/mL (703.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
-
Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
-
TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
-
Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
-
Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
-
Protocol For Protein Expression And Purification
Recombinant protein expression in Escherichia coli followed by purification of a His-tagged soluble protein by immobilized metal affinity chromatography (IMAC), with optional MBP fusion and TEV tag removal when the construct includes these elements. The biological readout is production of the encoded target protein, detected as an inducible band at the expected molecular mass by SDS-PAGE and quantified by total protein assay or chromatographic absorbance; the purification readout is enrichment of the target protein in elution fractions after selective binding of polyhistidine residues to immobilized Ni2+/metal-chelate resin and elution by imidazole-containing buffer. Expression is driven by an inducible bacterial expression system, commonly T7/lac-based, in which IPTG or lactose/auto-induction activates transcription and translation of the cloned gene; lower induction temperature, lower inducer concentration, induction timing, and solubility-enhancing fusion tags can influence the frac
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3451 mL | 11.7253 mL | 23.4505 mL | 58.6263 mL |
| 5 mM | 0.4690 mL | 2.3451 mL | 4.6901 mL | 11.7253 mL | |
| 10 mM | 0.2345 mL | 1.1725 mL | 2.3451 mL | 5.8626 mL | |
| 15 mM | 0.1563 mL | 0.7817 mL | 1.5634 mL | 3.9084 mL | |
| 20 mM | 0.1173 mL | 0.5863 mL | 1.1725 mL | 2.9313 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9380 mL | 2.3451 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7817 mL | 1.9542 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5863 mL | 1.4657 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1725 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9771 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0235 mL | 0.1173 mL | 0.2345 mL | 0.5863 mL |
Trilexium Related Classifications
HY-157800 Related Classifications
Powered by Bioz