Trimidox (hydrochloride)

Trimidox (hydrochloride)

Catalog Number:
L002373072APE
Mfr. No.:
APE-C4714
Price:
$212
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          CF 233 (hydrochloride); N,3,4,5-tetrahydroxy-benzenecarboximidamide, monohydrochloride
          CAS Number
          95933-75-8
          Molecular Formula
          C7H8N2O4·HCl
          Molecular Weight
          220.6
          Appearance
          A crystalline solid
          Purity
          98.00%
          Solubility
          ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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