All Photos(1)
(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, PF-6463922
C21H19FN6O2
Recommended Products
Assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -95 to -115°, c = 0.5 in methanol
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
SMILES string
NC1=C(O[C@@H](C2=C3C=CC(F)=C2)C)C=C(C4=C(C#N)N(C)N=C4CN(C)C3=O)C=N1
Biochem/physiol Actions
Lorlatinib (PF-06463922) is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against most known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. It is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
Legal Information
Sold for research purposes under agreement from Pfizer Inc.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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BMC pulmonary medicine, 18(1), 13-13 (2018-01-25)
Crizotinib is recommended as first-line therapy in ROS1-driven lung adenocarcinoma. However, the optimal first-line therapy for this subgroup of lung cancer is controversial according to the available clinical data. Here, we describe a 57-year-old man who was diagnosed with stage
Journal of medicinal chemistry, 57(11), 4720-4744 (2014-05-14)
Although crizotinib demonstrates robust efficacy in anaplastic lymphoma kinase (ALK)-positive non-small-cell lung carcinoma patients, progression during treatment eventually develops. Resistant patient samples revealed a variety of point mutations in the kinase domain of ALK, including the L1196M gatekeeper mutation. In
The Lancet. Oncology, 18(12), 1590-1599 (2017-10-28)
Most patients with anaplastic lymphoma kinase (ALK)-rearranged or ROS proto-oncogene 1 (ROS1)-rearranged non-small-cell lung cancer (NSCLC) are sensitive to tyrosine kinase inhibitor (TKI) therapy, but resistance invariably develops, commonly within the CNS. This study aimed to analyse the safety, efficacy
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