Crizotinib

Name: Crizotinib
Brand: Tocris Bioscience
SKU: 4368

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

Citations (36)

COA / SDS

Potent c-MET/ALK inhibitor

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Product Description
Licensing Information
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Potent c-MET/ALK inhibitor

Alternative Names

PF 02341066,PF 2341066

View all MET Inhibitors »

Product Description

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.

Product Specifications

Molecular Weight

450.34

Formula

C₂₁H₂₂Cl₂FN₅O

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

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

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	2eq.HCl	45.03	100
	DMSO	4.5	10

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 all 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

Calculators

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

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Reconstitution Calculator

Background References

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