Lorlatinib (acetate)
Product Specifications
UNSPSC Description
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively[1][2][3].
Target Antigen
Anaplastic lymphoma kinase (ALK); Apoptosis; ROS Kinase
Type
Reference compound
Related Pathways
Apoptosis;Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/lorlatinib-acetate.html
Smiles
CN1C(C#N)=C2C(CN(C)C(C3=C([C@@H](C)OC4=C(N)N=CC2=C4)C=C(F)C=C3)=O)=N1.OC(C)=O
Molecular Weight
466.46
References & Citations
[1]Zou HY, et al. PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.|[2]Johnson TW, et al. 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 lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem. 2014 Jun 12;57(11):4720-44.|[3]Zou HY, et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking PF-02341066-resistant ROS1 mutations. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-135509/Lorlatinib-acetate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-135509/
Clinical Information
Phase 4
CAS Number
1924207-18-0
Curated Selection
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