Product Pathways - Tyrosine Kinase / Adaptors
Crizotinib #4401
- Molecular Formula:
- C21H22Cl2FN5O
- Molecular Weight:
- 450.34 g/mol
- Purity:
- >99%
Directions for Use
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.
Western Blotting
Western blot analysis of extracts from KARPAS-299 cells, untreated or treated with crizotinib (1 hr) at the indicated concentrations, using Phospho-ALK (Tyr1604) Antibody #3341 (upper) or ALK (D5F3) XP® Rabbit mAb #3633 (lower).
Structure
Chemical structure of crizotinib.
Background
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).
- Zou, H.Y. et al. (2007) Cancer Res 67, 4408-17.
- Christensen, J.G. et al. (2007) Mol Cancer Ther 6, 3314-22.
Application References
Have you published research involving the use of our products? If so we'd love to hear about it. Please let us know!
For Research Use Only. Not For Use In Diagnostic Procedures.
