Crizotinib is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 2.5 mg in 5.55 ml DMSO. Working concentrations and length of treatments vary depending on the desired effect, but it is typically used at 0.1-1 µM for 2-6 h. Soluble in DMSO at 25 mg/ml with warming; very poorly soluble in water with maximum solubility ~10-20 µM.
|Molecular Weight||450.34 g/mol|
|Solubility||Soluble in DMSO and EtOH at 25mg/ml.|
Crizotinib, also known as PF-02341066, is a novel, ATP-competitive receptor kinase inhibitor, showing high specificity for c-Met and anaplastic lymphoma kinase (ALK) over 120 other diverse kinases (1,2). Researchers have shown that crizotinib inhibits c-Met phosphorylation and c-Met-dependent proliferation, migration, and invasion of human tumor cells in vitro (IC50 values of 5–20 nM) (1). Crizotinib is effective against the constitutively active oncogenic fusion protein nucleophosmin (NPM)-ALK, inhibiting its phosphorylation (mean IC50 of 24 nM), inhibiting cell growth, and inducing G1-S phase cell cycle arrest and apoptosis in the ALK-positive ALCL (anaplastic large-cell lymphoma) cell lines KARPAS-299 and SU-DHL-1 (2).
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