PF-2341066(Crizotinib);

cas# 877399-52-5;

purity:98%;

in stock!

Biological Activity of PF-2341066(Crizotinib):

Inhibitor of the catalytic activity of c-Met kinase and the NPM-ALK(nucleophosmin-

anaplastic lymphoma kinase) fusion protein.[1] A t(2;5) chromosomal translocation resulting in expression of an oncogenic kinase fusion protein known as NPM-ALK has been implicated in the pathogenesis of anaplastic large-cell lymphoma (ALCL). [2]

After incubation with PF-2341066, cells were washed once with HBSS supplemented

with 1 mmol/L Na3VO4 and protein lysates were generated. Subsequently, phosphorylation of ALK was assessed by a sandwich ELISA method using an immobilized anti–total-ALK antibody and an anti–phospho-ALK antibody (pY1604) as a detec ion antibody.

PF-2341066 inhibited NPM-ALKphosphorylation in Karpas299 or SU-DHL-1 ALCL cells (mean IC50 value=24 nM).

PF-2341066 potently inhibited cell proliferation, which was associated with G1-S–phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells (IC50 values=30 nM) but not ALK-negative lymphoma cells. The induction of apoptosis was confirmed using terminal deoxyribonucleotide transferase–mediated nick-end labeling and Annexin V staining (IC50 values=25–50 nM). [3]

References on PF-2341066(Crizotinib):

[1] Deininger M et al.Blood 2005, 105:2640–53

[2] Duyster J et al.Oncogene 2001, 20:5623–37

[3] James G. Christensen1 et al. Mol Cancer Ther December. 2007, 6:3314