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(S)-crizotinib

Catalog No. T6357   CAS 1374356-45-2
Synonyms: ent-crizotinib

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

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(S)-crizotinib Chemical Structure
(S)-crizotinib, CAS 1374356-45-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 64.00
10 mg In stock $ 97.00
25 mg In stock $ 162.00
50 mg In stock $ 239.00
100 mg In stock $ 372.00
1 mL * 10 mM (in DMSO) In stock $ 70.00
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Purity: 99.89%
Purity: 99.47%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description (S)-crizotinib (ent-crizotinib) (IC50 of 72 nM), an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.
Targets&IC50 MTH1:72 nM
In vitro In the SW480 colorectal cancer model, daily oral administration of 50mg/kg (S)-Crizotinib effectively inhibits tumor growth.
In vivo (S)-crizotinib activates DNA repair mechanisms in human colorectal cancer cells by inhibiting MTH1, thereby disrupting nucleotide pool homeostasis and further inducing an increase in DNA single-strand breaks.
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 1 year

Solubility Information

1eq. HCl: 9 mg/mL (20 mM)), Heating is recommended.

DMSO: 22.5 mg/mL (50 mM)

TargetMolReferences 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:
Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Bioactive Compounds Library Max Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library

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Keywords

(S)-crizotinib 1374356-45-2 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair MTH1 DNA/RNA Synthesis mutT inhibit nucleotide crizotinib (S) crizotinib homologue Inhibitor activity ent-crizotinib anticancer pool (S)-Crizotinib (S)crizotinib inhibitor

 

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