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Crizotinib
- PF-02341066 - PF-2341066
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C21H22Cl2FN5O
- MW: 450.34
Description
Crizotinib is a potent, selective and ATP-competitive c-Met/HGF receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 values of 4 nM for c-Met and 25 nM for ALK.
Crizotinib is a clinically validated kinase inhibitor used as a reference compound for MET-, ALK- and ROS1-driven oncogenic signaling. It is relevant for studying receptor tyrosine kinase addiction, fusion kinase biology and targeted cancer pharmacology.
Key Features
- Potent c-Met and ALK kinase inhibitor
- IC50: 4 nM for c-Met and 25 nM for ALK
- Reference compound for ALK-rearranged cancer models
- ATP-competitive receptor tyrosine kinase pharmacology
Applications
- MET/HGF signaling studies
- ALK and fusion kinase research
- Targeted oncology assay development
- Kinase selectivity and resistance models
Note: The opposite enantiomer, (S)-Crizotinib (Axon 2296), has been reported as an MTH1 inhibitor, whereas the R-enantiomer is inactive in that assay.
More Information
| Parent CAS No. | 877399-52-5 |
|---|---|
| Chemical Name | (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine |
| extra_info | . |
| SMILES | C1C(Cl)=C([C@H](OC2C=C(C3C=NN(C4CCNCC4)C=3)C=NC=2N)C)C(Cl)=C(F)C=1 |&1:4,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1 |
| InChiKey | KTEIFNKAUNYNJU-GFCCVEGCSA-N |
| CID | 11626560 |
| Short Description | MET/ALK inhibitor |
References
- A.T. Shaw et al. Crizotinib versus chemotherapy in advanced ALK-positive lung cancer. N. Engl. J. Med. 2013, 368, 2385-2394.
- HY Zou et al. An Orally Available Small-Molecule Inhibitor of c-Met, PF-2341066, Exhibits Cytoreductive Antitumor Efficacy through Antiproliferative and Antiangiogenic Mechanisms. Cancer Res. 2007, 67, 4408.
- SH Ou et al. Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification. J. Thor. Oncol. 2011, 6(5), 942-946.
- K.V. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, doi: 10.1038/nature13194. [Epub ahead of print]
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