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Submit ReviewPF 06463922
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% (HPLC)
Biological Activity for PF 06463922
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.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data for PF 06463922
| M. Wt | 406.41 |
| Formula | C21H19FN6O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1454846-35-5 |
| PubChem ID | 71731823 |
| InChI Key | IIXWYSCJSQVBQM-LLVKDONJSA-N |
| Smiles | C[C@@H](O3)C4=C(C=CC(F)=C4)C(N(C)CC1=NN(C)C(C#N)=C1C2=CC3=C(N)N=C2)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for PF 06463922
References for PF 06463922
References are publications that support the biological activity of the product.
Johnson et al (2014) Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lympho J.Med.Chem. 57 4720 PMID: 24819116
Zou et al (2015) PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc.Natl.Acad.Sci.U.S.A. 112 3493 PMID: 25733882
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Keywords: PF 06463922, PF 06463922 supplier, anaplastic, lymphoma, kinases, (ALK), inhibitors, inhibits, inhibition, ROS1, c-ros, oncogenes, cancer, PF06463922, Lorlatinib, ALK, 5640, Tocris Bioscience
1 Citation for PF 06463922
Citations are publications that use Tocris products. Selected citations for PF 06463922 include:
Fadeev et al (2018) ALKALs are in vivo ligands for ALK family receptor tyrosine kinases in the neural crest and derived cells. Proc Natl Acad Sci U S A 115 E630 PMID: 29317532
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