An ATP-competitive

PF-06463922 – 1 mg

Brand:
Cayman
CAS:
1454846-35-5
Storage:
-20
UN-No:
Non-Hazardous - /

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = i = 0.7 nM).{29757} It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).{29757,29756,29759} PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.{29757,29758} It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.{29756}  

 

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Description

An ATP-competitive, selective inhibitor of ALK (Ki = i = 0.7 nM) with strong activity against all known ALK and ROS1 mutants identified in patients; orally available with efficient blood-brain barrier penetration

Formal 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

Synonyms:  Lorlatinib

Molecular weight: 406.4

CAS: 1454846-35-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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