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Submit ReviewCrizotinib
Description: Potent c-MET/ALK inhibitor
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
Purity: ≥99% (HPLC)
Biological Activity for Crizotinib
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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data for Crizotinib
| M. Wt | 450.34 |
| Formula | C21H22Cl2FN5O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 877399-52-5 |
| PubChem ID | 11626560 |
| InChI Key | KTEIFNKAUNYNJU-GFCCVEGCSA-N |
| Smiles | ClC1=[C@@]([C@H](OC2=C(N)N=CC(C3=CN(C4CCNCC4)N=C3)=C2)C)C(Cl)=CC=C1F |
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.
Solubility Data for Crizotinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.5 | 10 | |
| 2eq.HCl | 45.03 | 100 |
Preparing Stock Solutions for Crizotinib
The following data is based on the product molecular weight 450.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.22 mL | 11.1 mL | 22.21 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 10 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for Crizotinib
References for Crizotinib
References are publications that support the biological activity of the product.
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
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
If you know of a relevant reference for Crizotinib, please let us know.
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Keywords: Crizotinib, Crizotinib supplier, c-MET, alk, anaplastic, lymphoma, kinases, antitumor, selective, potent, PF2341066, PF02341066, PF, 02341066, 2341066, MET, Receptors, ALK, 4368, Tocris Bioscience
9 Citations for Crizotinib
Citations are publications that use Tocris products. Selected citations for Crizotinib include:
Jan et al (2021) The tyrosine kinase inhibitor crizotinib influences blood glucose and mRNA expression of GLUT4 and PPARs in the heart of rats with experimental diabetes. Can J Physiol Pharmacol 99 635-643 PMID: 33201727
Maru et al (2019) Establishment and characterization of patient-derived organoids from a young patient with cervical clear cell carcinoma. Cancer Sci PMID: 31265190
Ayoub (2017) Crizotinib, a MET inhibitor, inhibits growth, migration, and invasion of breast cancer cells in vitro and synergizes with chemotherapeutic agents. Onco Targets Ther 10 4869 PMID: 29042798
Sullivan et al (2012) ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. FASEB J 8 646 PMID: 22660439
Zhu et al (2016) Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis. Oncogene 35 5388 PMID: 27109105
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
Alan M et al (2020) 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 Oncol Rep 44 2581-2594 PMID: 33125153
Gimenez-Xavier et al (2017) Genomic and Molecular Screenings Identify Different Mechanisms for Acquired Resistance to MET Inhibitors in Lung Cancer Cells. Mol Cancer Ther 16 1366 PMID: 28396363
Gimenez-Xavier et al (2018) Deep analysis of acquired resistance to FGFR1 inhibitor identifies MET and AKT activation and an expansion of AKT1 mutant cells. Oncotarget 9 31549 PMID: 30140389
Do you know of a great paper that uses Crizotinib from Tocris? Please let us know.
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