Trimidox (hydrochloride)
(Synonyms: CF 233 (hydrochloride)) 目录号 : GC16006A ribonucleotide reductase inhibitor
Cas No.:95933-75-8
Sample solution is provided at 25 µL, 10mM.
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.
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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