Crizotinib

Cat. No. 4368

Crizotinib C21H22Cl2FN5O [877399-52-5]

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Alternative Names: PF 02341066, PF 2341066

Chemical Name: 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine

Biological Activity

Potent inhibitor of c-MET and anaplastic lymphoma kinase (ALK) (cell IC50 values are 8.0 and 20 nM respectively). Selective for c-MET and ALK against >120 different kinases. Displays antitumor efficacy in multiple tumor models; inhibits c-MET-dependent proliferation, migration and invasion of human tumor cells in vitro. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
450.34
Formula:
C21H22Cl2FN5O
Solubility:
Soluble to 10 mM in DMSO and to 100 mM in 2eq.HCl
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
877399-52-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Cui et al (2011) Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J.Med.Chem. 54 6342. PMID: 21812414.

Christensen et al (2007) Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol.Cancer Ther. 6 3314. PMID: 18089725.

Zou et al (2007) An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 67 4408. PMID: 17483355.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Crizotinib include:

Qi et al (2011) Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res 71 1081. PMID: 21266357.

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View Related Products by Product Action

Keywords: Crizotinib, supplier, c-MET, alk, anaplastic, lymphoma, kinases, antitumor, selective, potent, PF2341066, PF02341066, Tocris Bioscience, ALK Inhibitor products

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