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

Trilexium  (Synonyms: TRX-E-009-1)

Cat. No.: HY-157800 Purity: 99.70%
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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.

Trilexium Chemical Structure

Trilexium Chemical Structure

CAS No. : 1983180-82-0

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5 mg USD 548 In-stock
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Based on 1 publication(s) in Google Scholar

Trilexium Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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].

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.

Trilexium Related Antibodies
In Vivo

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].

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.
Molecular Weight

426.43

Formula

C24H23FO6
CAS No.
Appearance

Solid

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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3451 mL 11.7253 mL 23.4505 mL
5 mM 0.4690 mL 2.3451 mL 4.6901 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Trilexium Related Classifications

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.

Keywords:

Trilexium1983180-82-0TRX-E-009-1Microtubule/TubulinApoptosisPARPCaspasepoly ADP ribose polymeraseHSJD-DIPG007melanomaA375BRAFV600Eanti cancerInhibitorinhibitorinhibit

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