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

Trimetrexate isethionate  (Synonyms: CI-898 isethionate)

目录号: HY-10373B
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摩尔计算器

Trimetrexate (CI-898) isethionate 是一种抗生素 (antibiotic)，也是一种有效的、具有口服活性的二氢叶酸还原酶 (DHFR) 抑制剂，减少 DNA 和 RNA 前体的产生并导致细胞死亡，对人 DHFR 和刚地弓形虫 (Toxoplasma gondii) DHFR 的 IC50 分别为 4.74 nM 和 1.35 nM。Trimetrexate isethionate 也能抑制多种癌细胞的生长。Trimetrexate isethionate 可用于卡氏肺孢子虫肺炎 (PCP) 和癌症的研究。

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Trimetrexate isethionate Chemical Structure

Trimetrexate isethionate Chemical Structure

CAS No. : 82935-04-4

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Trimetrexate isethionate 的其他形式现货产品:

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Trimetrexate isethionate 相关抗体

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  • 生物活性

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生物活性

Trimetrexate (CI-898) isethionate 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 isethionate can also inhibit the growth of various cancer cells. Trimetrexate isethionate can be used for researching Pneumocystis carinii pneumonia (PCP) and cancer[1][2][3][4][5].

IC50 & Target[1]

Toxoplasma

 

体外研究
(In Vitro)

Trimetrexate isethionate (0.1 μM; 18 h) completely inhibits proliferation of toxoplasma in murine macrophages[3].
Trimetrexate isethionate (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.

Trimetrexate isethionate 相关抗体:

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.
体内研究
(In Vivo)

Trimetrexate (180 mg/kg or 30 mg/kg; p.o. or i.p.; daily) isethionate 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) isethionate 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.
Clinical Trial
分子量

495.55

Formula

C21H29N5O7S
CAS 号
中文名称

三甲曲沙羟乙基磺酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Trimetrexate isethionate 相关分类

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  • 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:

Trimetrexate82935-04-4CI-898三甲曲沙羟乙基磺酸盐CI898CI 898Dihydrofolate reductase (DHFR)AntibioticAntifolateParasiteBacterialDNA/RNA SynthesisPneumocystis carinii pneumoniaPCPDHFRToxoplasma gondiianticancerInhibitorinhibitorinhibit

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