Catalog No.S7505

(S)-crizotinib Chemical Structure

Molecular Weight(MW): 450.34

(S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM in a cell-free assay.

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  • (B) Inhibition of ALK phosphorylation by alectinib in the Ba/F3 cell lines expressing mutated EML4-ALK. Cells were treated with alectinib or crizotinib for 2 h at the indicated concentrations. Phosphorylated ALK (Tyr 1604), ALK, and β-actin were detected by immunoblot analysis using antibodies to each of them.

    Cancer Letters, 2014, 35(2):215-221.. (S)-crizotinib purchased from Selleck.

    (A) A dose-response curve of MTH1 inhibition by a positive control: (S)-crizotinib inhibited MTH1 with an IC50 of 0.5 μM;

    Onco Targets Ther, 2015, 8: 3649-3664.. (S)-crizotinib purchased from Selleck.

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Choose Selective MTH1 Inhibitors

Biological Activity

Description (S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM in a cell-free assay.
Features MTH1 (NUDT1)- selective inhibitor.
MTH1 [1]
(Cell-free assay)
72 nM
In vitro

(S)-crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single-strand breaks, and activates DNA repair in human colon carcinoma cells. [1]

In vivo (S)-Crizotinib (50 mg/kg, orally, daily) impairs tumor growth in an SW480 colon carcinoma xenograft model. [1]


Kinase Assay:


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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:


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  • Cell lines: PANC1 and SW480 cells
  • Concentrations: ~5 礛
  • Incubation Time: 7-10 days
  • Method:

    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)
Animal Research:


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  • Animal Models: SW480 colon carcinoma xenograft mouse model.
  • Formulation: ~50 mg/kg daily
  • Dosages: 1% DMSO, 10% ethanol, 10% Cremophor, 10% Tween 80, 69% PBS
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 42 mg/mL warmed (93.26 mM)
Ethanol 22 mg/mL (48.85 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.34


CAS No. 1374356-45-2
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Could you tell me whether this product represents the pure R-form of crizotinib, or is the the racemic Crizotinib, so a mixture of the S- and the R-form?

  • Answer:

    Our S1068 Crizotinib is R enantiomer, and S7505 is S enantiomer. Normally, Crizotinib refers to the R enantiomer

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID