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(S)-Crizotinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(S)-Crizotinib图片
CAS NO:1374356-45-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
ent-crizotinib
产品介绍
(S)-Crizotinib 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。

产品描述

(S)-crizotinib(IC50 of 72 nM), an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

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。

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.

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)

Cas No.

1374356-45-2

分子式

C21H22Cl2FN5O

分子量

450.34

别名

ent-crizotinib

储存和溶解度

1eq. HCl:9 mg/mL (20 mM)),with gentle warming
DMSO:22.5 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years