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: 98.63%
COA 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 290 在庫あり
Solution
10 mM * 1 mL in DMSO USD 290 在庫あり
Solid
5 mg USD 264 在庫あり
10 mg USD 480 在庫あり
50 mg USD 1680 在庫あり
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

This product is a controlled substance and not for sale in your territory.

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

 

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].

MedChemExpress (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].

MedChemExpress (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
Appearance

Solid

Color

Light yellow to green yellow

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:  50% PEG300    50% Saline

    Solubility: 40 mg/mL (108.28 mM); Suspended solution; Need ultrasonic

  • 2.

    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

  • 3.

    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 MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.22%

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