Crizotinib, c-MET and ALK receptor tyrosine kinase inhibitor (ab218605)

Overview

  • Product name

    Crizotinib, c-MET and ALK receptor tyrosine kinase inhibitor
  • Description

    Potent, selective c-MET and ALK receptor tyrosine kinase inhibitor
  • Alternative names

    • PF 02341066
    • PF 2341066
    • PF02341066
    • Xalkori
  • Biological description

    Potent, ATP-competitive inhibitor of c-MET and anaplastic lymphoma kinase (ALK) receptor tyrosine kinases (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.

  • Purity

    > 98%
  • CAS Number

    877399-52-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
  • Molecular weight

    450.34
  • Molecular formula

    C21H22Cl2FN5O
  • PubChem identifier

    11626560
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 10 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C[C@H](C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N
  • Source

    Synthetic

References

This product has been referenced in:

  • Tanizaki J  et al. MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations. J Thorac Oncol 6:1624-31 (2011). Read more (PubMed: 21716144) »
  • Cui JJ  et al. 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 54:6342-63 (2011). Read more (PubMed: 21812414) »
  • Zou HY  et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res 67:4408-17 (2007). Read more (PubMed: 17483355) »
  • Christensen JG  et al. 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 6:3314-22 (2007). Read more (PubMed: 18089725) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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