KIN-59
(Synonyms: 5'-O-三苯甲基-肌苷,5’-O-Tritylinosine) 目录号 : GC16460An inhibitor of TPase
Cas No.:4152-77-6
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
KIN59, the purine riboside derivative, is a noncompetitive inhibitor against human and bacterial recombinant TPase [1]. TPase is an enzyme with an important role in the pyrimidine nucleoside salvage pathway and the inactivation of cytotoxic pyrimidine nucleoside analogues. TPase also recognizes several nucleoside analogues clinically used as antiviral or anti-tumor agents [1]. Overexpression of TPase has been observed in many solid tumors [1].
In vitro: In the purified E. coli and human TPase, KIN59 inhibited the E. coli and human TPases in a reversible or irreversible manner, with the IC50 of 44 ± 3 and 67 ± 20 M, respectively. KIN59 was a potent inhibitor of E. coli TPase with Ki values of 39 M against dThd and 146 M against phosphate, resulting in Ki /Km values of 0.039 and 0.10, respectively. KIN59 induced the formation of an avascular area around and inside the sponge. In the CAM assay, KIN59 completely prevented TPase-stimulated blood vessel formation, without any visible side effects [1]. KIN59 was active against TPase-induced angiogenesis in the chorioallantoic membrane assay [1].
Reference:
[1] Liekens S, Hernández A I, Ribatti D, et al. The nucleoside derivative 5′-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action[J]. Journal of Biological Chemistry, 2004, 279(28): 29598-29605.
| Cas No. | 4152-77-6 | SDF | |
| 别名 | 5'-O-三苯甲基-肌苷,5’-O-Tritylinosine | ||
| 化学名 | 5'-O-(triphenylmethyl)-inosine | ||
| Canonical SMILES | O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=CNC3=O)O[C@@H]1COC(C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6 | ||
| 分子式 | C29H26N4O5 | 分子量 | 510.5 |
| 溶解度 | ≤0.3mg/ml in ethanol;16mg/ml in DMSO;5mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9589 mL | 9.7943 mL | 19.5886 mL |
| 5 mM | 0.3918 mL | 1.9589 mL | 3.9177 mL |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9589 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。