Crizotinib

Pricing Availability Delivery Time Qty
Cat.No. 4368 - Crizotinib | C21H22Cl2FN5O | CAS No. 877399-52-5
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)
Datasheet
Citations (3)
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 450.34. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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View Related Products by Product Action

View all ALK Inhibitors

Keywords: Crizotinib, supplier, c-MET, alk, anaplastic, lymphoma, kinases, antitumor, selective, potent, PF2341066, PF02341066, PF, 02341066, PF, 2341066, MET, Receptors, ALK, ALK, Tocris Bioscience

3 Citations for Crizotinib

Citations are publications that use Tocris products. Selected citations for Crizotinib include:

Sullivan et al (2012) ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. FASEB J 8 646 PMID: 22660439

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

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


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