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- 2026年07月07日
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- CAS号：
1374356-45-2
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥391.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥190.0 |
| 规格： | 5mg | 产品价格： | ￥396.0 |
| 规格： | 10mg | 产品价格： | ￥596.0 |
| 规格： | 25mg | 产品价格： | ￥984.0 |
| 规格： | 50mg | 产品价格： | ￥1456.0 |
| 规格： | 100mg | 产品价格： | ￥2304.0 |
Product Introduction
Bioactivity
| 名称 | (S)-crizotinib |
| 描述 | (S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib. |
| 细胞实验 | One day before treatment, cells are seeded per well in six-well plates and incubated for 24 h. The next day DMSO (equal to highest amount of compound dilution, maximum 0.2%) or compounds in increasing concentrations were added and cells incubated at 37 °C, 5% CO2, for 7-10 days. After washing with PBS, cells are fixed with ice-cold methanol, stained with crystal violet solution (0.5% in 25% methanol) and left to dry overnight. For quantification of results, ultraviolet absorbance of crystal violet is determined at 595 nm following solubilisation by 70% ethanol. Data are analysed using nonlinear regression analysis using the GraphPad Prism software. (Only for Reference) |
| 激酶实验 | MTH1 catalytic assay: Half-maximal inhibitory concentrations (IC50) are determined using a luminescence-based assay with some minor modifications. Briefly, serial dilutions of compounds are dissolved in assay buffer (100?mM Tris-acetate pH?7.5, 40?mM NaCl and 10?mM Mg(OAc)2 containing 0.005% Tween-20 and 2?mM dithiothreitol (DTT). Upon addition of MTH1 recombinant protein (final concentration 2?nM), plates are incubated on a plate shaker for 15?min at room temperature. After addition of the substrate dGTP (final concentration 100?μM), 8-oxo-dGTP (final concentration 13.2?μM), or 2-OH-dATP (final concentration 8.3?μM) the generation of pyrophosphate (PPi) as a result of nucleotide triphosphate hydrolysis by MTH1 is monitored over a time course of 15?min using the PPi Light Inorganic Pyrophosphate Assay kit. IC50 values are determined by fitting a dose-response curve to the data points using nonlinear regression analysis using the GraphPad Prism software. |
| 体外活性 | 在SW480 结肠癌模型中,每天口服 50?mg/kg(S)-Crizotinib能够阻碍肿瘤的生长. |
| 体内活性 | (S)-crizotinib能够激活人结肠癌细胞中DNA修复机制,它抑制MTH1从而破坏核苷酸库的稳态,进一步诱导DNA单链断裂的增加。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.22 mM), Sonication is recommended. 1eq. HCl : 9 mg/mL (19.98 mM), Heating is recommended. DMSO : 22.5 mg/mL (49.96 mM), Sonication is recommended. |
| 关键字 | RNASynthesis | RNA Synthesis | pool | nucleotide | mutT | MTH1 | Inhibitor | inhibit | homologue | DNASynthesis | DNA/RNA Synthesis | DNA Synthesis | crizotinib | Apoptosis | anticancer | activity | (S)-Crizotinib | (S)crizotinib | (S) crizotinib |
| 相关产品 | Formamide | Urea | Guanidine hydrochloride | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Stavudine | Tamoxifen | Thymidine |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Aging Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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文献和实验上有两个或两个以上相同杂原子时，应从连接有氢或取代基的杂原子开始编号，并使这些杂原子所在位次的数字之和为最小。环上有不同杂原子时，则按氧、硫、氮为序编号。例如： 表19－1 常用杂环化合物的构造式和名称 另有特殊编号的，如嘌呤等（见表19-1）。 二、杂环化合物的结构 五元杂环化合物呋喃、噻吩、吡咯的结构和苯相类似。构成环的四个碳原子和杂原子（N，S，O）均为sp2杂化状态
甾类（化合物）17α-羟化酶 steroid 17α－hy- droxylase，s eroid 17α-monooxygeoase
甾类（化合物）17α-羟化酶 steroid 17α－hy- droxylase，s eroid 17α-monooxygeoase 存在于睾丸、肾上腺的微粒体部分。是一种在甾类分子的17α位置上引入羟基的酶。EC1、14、99、9。需要有分子态氧和NADPH存在，与P－450有关。例如将黄体酮和孕（甾）烯醇酮各自成为17α-羟基黄体酮和17α-羟基孕烯醇酮。在鼠的肾上腺中不存在此酶。
S－腺苷甲硫氨酸 S－ adenosylmethionine 亦称活性甲硫氨酸，在生物体内由 ATP与甲硫氨酸在甲硫氨酸活化酶的作用下合成。甲硫键是高能键，另外其丙基胺部分也加入到多胺化合物中。当胆碱、肌酸及其它甲基化合物生成时它作为甲基供体而起作用。认为甲硫氨酸的分解也经过此物质。
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