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(S)-crizotinib

Catalog No. T6357 CAS 1374356-45-2

Synonyms: ent-crizotinib

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

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(S)-crizotinib, CAS 1374356-45-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	(S)-crizotinib（IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.
Targets&IC50	MTH1:72 nM
Kinase Assay	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.
Cell Research	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)

Synonyms	ent-crizotinib
Molecular Weight	450.34
Formula	C21H22Cl2FN5O
CAS No.	1374356-45-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

1eq. HCl: 9 mg/mL (20 mM)), with gentle warming

DMSO: 22.5 mg/mL (50 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Huber KV, et al. Nature. 2014 , 508(7495), 222-227.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Endoplasmic Reticulum Stress Compound Library Anti-Cancer Metabolism Compound Library Inhibitor Library DNA Damage & Repair Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library FDA-Approved Drug Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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