PF 06463922

Catalog # Availability Size / Price Qty
5640/10
5640/50
Cat.No. 5640 - PF 06463922 | C21H19FN6O2 | CAS No. 1454846-35-5
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Description: High affinity and selective ALK and ROS1 inhibitor
Alternative Names: Lorlatinib

Chemical Name: (10R)-7-Amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile

Purity: ≥98%

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Biological Activity

High affinity and selective ALK and ROS1 inhibitor (Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively). Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.

Technical Data

M.Wt:
406.41
Formula:
C21H19FN6O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1454846-35-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

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