化合物 (S)-crizotinib|T6357|TargetMol

(S)-crizotinib
1374356-45-2

￥218 1mg 起订

￥297 2mg 起订

￥496 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 (S)-crizotinib

英文名称：: (S)-crizotinib

CAS号：: 1374356-45-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.89%

产品类别：: 抑制剂

货号：: T6357

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.
溶解度	1eq. HCl : 9 mg/mL (20 mM)), Heating is recommended. DMSO : 22.5 mg/mL (50 mM)
关键字	mutT \| inhibit \| nucleotide \| crizotinib \| Apoptosis \| (S) crizotinib \| homologue \| Inhibitor \| activity \| anticancer \| pool \| (S)-Crizotinib \| (S)crizotinib \| DNA/RNA Synthesis
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相关库	抑制剂库 \| 抗癌上市药物库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

ent-crizotinib|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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