2. Cell Cycle/DNA Damage Anti-infection
  3. Antifolate Bacterial
  4. Trimetrexate glucuronate

Trimetrexate glucuronate  (Synonyms: CI-898 glucuronate)

Cat. No.: HY-103396 Purity: 98.09%
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Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.

For research use only. We do not sell to patients.

Trimetrexate glucuronate Chemical Structure

Trimetrexate glucuronate Chemical Structure

CAS No. : 82952-64-5

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5 mg USD 264 In-stock
10 mg USD 480 In-stock
50 mg USD 1680 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Trimetrexate glucuronate:

Trimetrexate glucuronate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia[1][2].

In Vitro

Trimetrexate glucuronate (0.05-1 μM 6 h) results in a decrease in adenosine and guanosine acids and a significant increase in the pyrimidine nucleotide such as CTP, UTP of WI-L2 human lymphoblastoid cells in a dose-dependent manner[1].
Trimetrexate glucuronate (1 μM, 2 h) can reduce the level of dTTP by 29%, also decrease in the dGTP and dATP, while cause extensive inhibition of deoxyuridine incorporation into DNA in L1210 mouse leukemia cells[1].

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

Trimetrexate glucuronate Related Antibodies
In Vivo

Trimetrexate glucuronate (i.p., 100-225 mg/kg, daily, day 1, 5, 9) has antitumor activity in inbred DBA/2 mice with L1210 leukemia[1].

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

Animal Model: Inbred DBA/2 mice with L1210 leukemia[1]
Dosage: 100, 150, 225 mg/kg
Administration: Intraperitoneal injection; daily; day 1, 5, 9
Result: Showed the maximum lifespan T/C value of 171%.
Animal Model: C57BL/6 mice with M5076 tumor[1]
Dosage: 38, 62 mg/kg
Administration: Intraperitoneal injection; daily; 1-9 days
Result: Showed toxic (>10% early deaths) at high dose of 62 mg/kg and inactive (Lifespan T/C <130%) at lower dose of 38 mg/kg.
Clinical Trial
Molecular Weight

563.56

Formula

C25H33N5O10
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C[C@@H]([C@H]([C@@H]([C@@H](C(O)=O)O)O)O)O.NC1=NC(N)=C2C(C)=C(CNC3=CC(OC)=C(OC)C(OC)=C3)C=CC2=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (177.44 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 1.7744 mL 8.8722 mL 17.7443 mL
5 mM 0.3549 mL 1.7744 mL 3.5489 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 (sealed storage, away from moisture). 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: 2.5 mg/mL (4.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 4 mg/mL (7.10 mM); Clear solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  0.5% CMC/saline water

    Solubility: 2.5 mg/mL (4.44 mM); Suspended solution; Need ultrasonic

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 (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 1.7744 mL 8.8722 mL 17.7443 mL 44.3608 mL
5 mM 0.3549 mL 1.7744 mL 3.5489 mL 8.8722 mL
10 mM 0.1774 mL 0.8872 mL 1.7744 mL 4.4361 mL
15 mM 0.1183 mL 0.5915 mL 1.1830 mL 2.9574 mL
20 mM 0.0887 mL 0.4436 mL 0.8872 mL 2.2180 mL
25 mM 0.0710 mL 0.3549 mL 0.7098 mL 1.7744 mL
30 mM 0.0591 mL 0.2957 mL 0.5915 mL 1.4787 mL
40 mM 0.0444 mL 0.2218 mL 0.4436 mL 1.1090 mL
50 mM 0.0355 mL 0.1774 mL 0.3549 mL 0.8872 mL
60 mM 0.0296 mL 0.1479 mL 0.2957 mL 0.7393 mL
80 mM 0.0222 mL 0.1109 mL 0.2218 mL 0.5545 mL
100 mM 0.0177 mL 0.0887 mL 0.1774 mL 0.4436 mL
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Trimetrexate glucuronate 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:

Trimetrexate glucuronate82952-64-5CI-898 glucuronateAntifolateBacterialfolic aciddihydrofolate reductasepurine nucleotidesthymidylateanti-tumorInhibitorinhibitorinhibit

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