Crizotinib

Name: Crizotinib
Brand: Tocris Bioscience
SKU: 4368

Tocris Bioscience, part of Bio-Techne | Catalog # 4368

Citations (28)

COA / SDS

Potent c-MET/ALK inhibitor

Key Product Details

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)
Molecular Weight:	450.34

View Full Technical Details for Crizotinib

Technical Data
Citations

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 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	11.10 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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References for Crizotinib

References are publications that support the biological activity of the product.

Zou An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 2007 PMID: 17483355
Cui 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. 2011 PMID: 21812414
Christensen 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. 2007 PMID: 18089725