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Trimidox (hydrochloride) Sale

(Synonyms: CF 233 (hydrochloride)) 目录号 : GC16006

A ribonucleotide reductase inhibitor

Trimidox (hydrochloride) Chemical Structure

Cas No.:95933-75-8

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5mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Description

Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor [1][2][3].

Ribonucleotide reductase is the rate-limiting enzyme for de novo DNA synthesis. This enzyme is linked with proliferation and malignant transformation, and is a common target for cancer chemotherapy [1][2].

Trimidox (hydrochloride) is a specific ribonucleotide reductase inhibitor. Trimidox inhibited the activity of ribonucleotide reductase in extracts of L1210 cells with IC50 value of 5 μM. Trimidox was cytotoxic to L1210 cells with IC50 value of 7.5 μM [3]. In human promyelocytic leukemia HL-60 cells, Trimidox inhibited cell growth with IC50 value of 35 μmol/L. Trimidox (50 μmol/L) reduced deoxyguanosine triphosphate (dGTP) and deoxycytidine triphosphate (dCTP) pools to 24% and 39% of control values, respectively. Trimidox and tiazofurin produced synergistic growth inhibitory activity, suggesting trimidox in combination with tiazofurin might be useful in the treatment of leukemia [1]. In several human leukaemia cell lines, Trimidox induced apoptosis, significantly increased cytochrome c release and activated caspase-3 and -9 [2].

In mice bearing intraperitoneally transplanted L1210 leukemia, Trimidox significantly increased the life span in a dose-dependent way [3].

References:
[1].  Szekeres T, Fritzer M, Strobl H, et al. Synergistic growth inhibitory and differentiating effects of trimidox and tiazofurin in human promyelocytic leukemia HL-60 cells. Blood. 1994 Dec 15;84(12):4316-21.
[2].  Kanno S, Uwai K, Tomizawa A, et al. Trimidox induces apoptosis via cytochrome c release in NALM-6 human B cell leukaemia cells. Basic Clin Pharmacol Toxicol. 2006 Jan;98(1):44-50.
[3].  Szekeres T1, Gharehbaghi K, Fritzer M, et al. Biochemical and antitumor activity of trimidox, a new inhibitor of ribonucleotide reductase. Cancer Chemother Pharmacol. 1994;34(1):63-6.

化学性质

Cas No. 95933-75-8 SDF
别名 CF 233 (hydrochloride)
化学名 N,3,4,5-tetrahydroxy-benzenecarboximidamide, monohydrochloride
Canonical SMILES Cl.ONC(=N)c1cc(O)c(O)c(O)c1
分子式 C7H8N2O4 • HCl 分子量 220.6
溶解度 ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 4.5331 mL 22.6655 mL 45.3309 mL
5 mM 0.9066 mL 4.5331 mL 9.0662 mL
10 mM 0.4533 mL 2.2665 mL 4.5331 mL
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