Crizotinib

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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 (9)
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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View Related Products by Product Action

View all ALK Inhibitors

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:

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


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