1. Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
    Anti-infection
  2. Dihydrofolate reductase (DHFR)
    Antibiotic
    Antifolate
    Parasite
    Bacterial
    DNA/RNA Synthesis
  3. Trimetrexate

Trimetrexate (Synonyms: CI-898)

製品番号: HY-10373 純度: 99.45%
取扱説明書

Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer.

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Trimetrexate 構造式

Trimetrexate 構造式

CAS 番号 : 52128-35-5

容量 価格(税別) 在庫状況 数量
Solution
10 mM * 1 mL in DMSO USD 290 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 290 在庫あり
Estimated Time of Arrival: December 31
Solid
5 mg USD 264 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 480 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1680 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

Other Forms of Trimetrexate:

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製品説明

Trimetrexate (CI-898) is an antibiotic, also a potent and orally active dihydrofolate reductase (DHFR) inhibitor, reducing the production of DNA and RNA precursors and leading to cell death, with IC50 values of 4.74 nM and 1.35 nM for human DHFR and Toxoplasma gondii DHFR. Trimetrexate can also inhibit the growth of various cancer cells. Trimetrexate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].

IC50 & Target[1]

Toxoplasma gondii

 

体外実験

Trimetrexate (0.1 μM, 18 h) completely inhibits proliferation of toxoplasma in murine macrophages[3].
Trimetrexate (1 μM) can cross the toxoplasma cell membrane and rapidly reaches high intracellular concentrations (108 pmol/107 cells within 10 min) [3].
Trimetrexate (0.1 mM; 24 h) inhibits cell growth by 50-60% in SNU-C4 and NCI-H630 cell lines[5].
Trimetrexate (1 and 10 mM; 24 h) produces lethality and inhibits DHFR in C4 cells[5].

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

Cell Proliferation Assay[5]

Cell Line: SNU-C4 and NCI-H630
Concentration: 0.1 mM
Incubation Time: 24 h
Result: Inhibited cell growth by 50-60% in both cell lines.

Cell Proliferation Assay[5]

Cell Line: C4 cells
Concentration: 1 and 10 mM
Incubation Time: 24 h
Result: Produced 42% and 50% lethality at 1 and 10 mM, respectively.
体内実験

Trimetrexate (180 mg/kg or 30 mg/kg; p.o. or i.p.; daily) extends the median survival of the toxoplasma infected mice and shows antitoxoplasma activity[3]. Trimetrexate (0-30 mg/kg; i.v.; once daily for 5days) shows chronic toxicity in rats[4].

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

Animal Model: Toxoplasma infected female BALB/c mice weighing about 20 g[3]
Dosage: 180 mg/kg or 30 mg/kg
Administration: 180 mg/kg per day orally in the drinking water or 30 mg/kg per day i.p.
Result: Extended the median survival of the infected mice to 10 d (p.o.) or 19 d (i.p.).
Animal Model: Charles River Wistar Crl(WI)BR rats weighing approximately 150 to 200 g[4]
Dosage: 0, 1, 10, or 30 mg/kg
Administration: Intravenous injection, once daily for 5 consecutive days followed by a 23-day recovery period
Result: Showed chronic toxicity, the testicular changes persisting during the course of multiple cycles of dosing were not reversible within 21 days, but required an additional 56 days for essentially complete recovery.
臨床実験
分子量

369.42

分子式

C19H23N5O3

CAS 番号
SMILES

NC1=C(C(C)=C2CNC3=CC(OC)=C(OC)C(OC)=C3)C(C=C2)=NC(N)=N1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 61.5 mg/mL (166.48 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7069 mL 13.5347 mL 27.0695 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are available by MCE.
純度とドキュメンテーション

純度: 99.45%

参考文献
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製品名:
Trimetrexate
製品番号:
HY-10373
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