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PF-2341066

Cat. No. M1765
PF-2341066 Structure
Synonym:

Crizotinib

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 120 In stock
100mg USD 200 In stock
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Quality Control
Biological Activity

PF-2341066 (Crizotinib) is a potent, orally bioavailable, ATP-competitive small-molecule inhibitor of c-Met kinase and ALK (anaplastic lymphoma kinase) with IC50 values to be 4 and 25 nM for C-Met and ALK resepectively.PF-2341066 (Crizotinib) 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).

Protocol
Cell Experiment
Cell lines Karpas299, SUDHL-1, or U-937 cells
Preparation method Cell Proliferation/Survival Assays. Cells were seeded in 96-well plates at low density at 37°C in medium supplemented with 10% FBS (growth medium) and after 24 h were switched to low serum medium (2% FBS). Designated concentrations of PF-2341066 were added to each well and cells were incubated at 37°C for 72 h. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay (Promega) was done to determine the relative cell numbers. IC50 values were calculated by concentration-response curve fitting using a Microsoft Excel–based four-parameter analytic method.
Concentrations 0~1µM
Incubation time 72h
Animal Experiment
Animal models S.c. Xenograft Models in Athymic Mice
Formulation sterile water
Dosages 100mg/kg daily
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 450.34
Formula C21H22Cl2FN5O
CAS Number 877399-52-5
Purity 98.62%
Solubility DMSO ≥23 mg/mL
Storage at -20°C
References

Brentuximab vedotin and crizotinib in anaplastic large-cell lymphoma.
Foyil KV, et al. Cancer J. 2012 Sep;18(5):450-6. PMID: 23006951.

Crizotinib for the Treatment of ALK-Rearranged Non-Small Cell Lung Cancer: A Success Story to Usher in the Second Decade of Molecular Targeted Therapy in Oncology.
Ou SH, et al. Oncologist. 2012 Sep 18. PMID: 22989574.

Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study.
Camidge DR, et al. Lancet Oncol. 2012 Oct;13(10):1011-9. PMID: 22954507.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-2341066, Crizotinib supplier, c-Met, inhibitors

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