Triapine
(Synonyms: [(3-氨基吡啶-2-基)亚甲基氨基]硫脲) 目录号 : GC17897
核糖核苷酸还原酶抑制剂
Cas No.:236392-56-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Wild-type (KB) and HU-resistant (KB/HU) human KB nasopharyngeal carcinoma cells. |
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Preparation method |
The solubility of this compound in DMSO is > 83.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
37oC |
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Applications |
Triapine is found to be a much more potent inhibitor of the enzyme than HU regardless of the cellular source of the enzyme, with a comparable inhibition at roughly a 1000-old lower concentration of Triapine than HU. |
| Animal experiment [1]: | |
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Animal models |
Mice xenografts of murine M109 lung carcinoma and the human A2780 ovarian carcinoma. |
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Dosage form |
i.p. or i.v. bolus injection (0.01 mL/g) |
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Preparation method |
Triapine in 0.9% NaCl |
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Applications |
Triapine significantly inhibits the growth in mice of the M109 lung carcinoma, the twice daily schedule produces tumor growth delays of 10 days compared to untreated control animals. Growth of the human A2780 ovarian carcinoma xenograft in nude mice is also significantly inhibited by Triapine, at 8 and 10 mg/kg given on a twice daily schedule. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Finch RA, Liu M, Grill SP et al. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91. | |
Triapine is a potent inhibitor of ribonucleotide reductase activity with IC50 value of 1.6 μM for various of tumor cell lines [1].
Triapine has been reported to inhibit ribonucleotide reductase activity. Triapine has shown its antineoplastic activity by inhibiting DNA synthesis and repair. In addition, Triapine has been revealed to inhibit the growth of the murine M109 lung carcinoma and human A2780 ovarian carcinoma xenografts in nude mice. Moreover, Triapine was active against the L1210 leukemia over a broad range of dosages and was curative for the M109 lung carcinoma and human A2780 ovarian carcinoma xenograft mice. [1, 2]
References:
[1]. Jennifer J. Knox, Sebastien J. Hotte, Christian Kollmannsberger, Eric Winquist, Bryn Fisher, Elizabeth A. Eisenhauer .Phase II study of Triapine® in patients with metastatic renal cell carcinoma: a trial of the National Cancer Institute of Canada Clinical Trials Group (NCIC IND.161). nvestigational New Drugs .October 2007, Volume 25, Issue 5, pp 471-477
[2]Finch RA1, Liu M, Grill SP, Rose WC, Loomis R, Vasquez KM, Cheng Y, Sartorelli AC. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91
| Cas No. | 236392-56-6 | SDF | |
| 别名 | [(3-氨基吡啶-2-基)亚甲基氨基]硫脲 | ||
| 化学名 | [(E)-(3-aminopyridin-2-yl)methylideneamino]thiourea | ||
| Canonical SMILES | C1=CC(=C(N=C1)C=NNC(=S)N)N | ||
| 分子式 | C7H9N5S | 分子量 | 195.24 |
| 溶解度 | ≥ 83.3mg/mL in DMSO | 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 | 5.1219 mL | 25.6095 mL | 51.219 mL |
| 5 mM | 1.0244 mL | 5.1219 mL | 10.2438 mL |
| 10 mM | 0.5122 mL | 2.561 mL | 5.1219 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。