Crizotinib
Chemical Name: 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
Purity: ≥99%
Biological Activity
Crizotinib is a 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines
A Stanley, GH Ashrafi, AM Seddon, H Modjtahedi
Sci Rep, 2017;7(1):3964. -
Deregulated hepsin protease activity confers oncogenicity by concomitantly augmenting HGF/MET signalling and disrupting epithelial cohesion.
Tervonen T, Belitskin D, Pant S, Englund J, Marques E, Ala-Hongisto H, Nevalaita L, Sihto H, Heikkila P, Leidenius M, Hewitson K, Ramachandra M, Moilanen A, Joensuu H, Kovanen P, Poso A, Klefstrom J
Oncogene, 2015;0(0):ePub. -
Acquired resistance to anti-EGFR mAb ICR62 in cancer cells is accompanied by an increased EGFR expression, HER-2/HER-3 signalling and sensitivity to pan HER blockers.
Khelwatty S, Essapen S, Seddon A, Fan Z, Modjtahedi H
Br J Cancer, 2015;113(7):1010-9.
Product Datasheets
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Citations for Crizotinib
The citations listed below are publications that use Tocris products. Selected citations for Crizotinib include:
9 Citations: Showing 1 - 9
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The tyrosine kinase inhibitor crizotinib influences blood glucose and mRNA expression of GLUT4 and PPARs in the heart of rats with experimental diabetes.
Authors: Jan Et al.
Can J Physiol Pharmacol 2021;99:635-643
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Synergistic activity of agents targeting growth factor receptors, CDKs and downstream signaling molecules in a panel of pancreatic cancer cell lines and the identification of antagonistic combinations: Implications for future clinical trials in pancreatic
Authors: Alan M Et al.
Oncol Rep 2020;44:2581-2594
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Establishment and characterization of patient-derived organoids from a young patient with cervical clear cell carcinoma.
Authors: Maru Et al.
Cancer Sci 2019;
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Deep analysis of acquired resistance to FGFR1 inhibitor identifies MET and AKT activation and an expansion of AKT1 mutant cells.
Authors: Gimenez-Xavier Et al.
Oncotarget 2018;9:31549
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Genomic and Molecular Screenings Identify Different Mechanisms for Acquired Resistance to MET Inhibitors in Lung Cancer Cells.
Authors: Gimenez-Xavier Et al.
Mol Cancer Ther 2017;16:1366
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Crizotinib, a MET inhibitor, inhibits growth, migration, and invasion of breast cancer cells in vitro and synergizes with chemotherapeutic agents.
Authors: Ayoub
Onco Targets Ther 2017;10:4869
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Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis.
Authors: Zhu Et al.
Oncogene 2016;35:5388
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ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53.
Authors: Sullivan Et al.
FASEB J 2012;8:646
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Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors.
Authors: Qi Et al.
Cancer Res 2011;71:1081
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