PF-06463922 [1454846-35-5]

Catalog number: HY-12215_5mg
Brand: MedChem Express
Packing: 5 mg
Other sizes: 10 mM
10 mg
25 mg
50 mg
100 mg
Price: € 102.00
Expected delivery time: 10 days

Product specifications for - PF-06463922 [1454846-35-5]

Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 1454846-35-5
Purity: >98%
Molecular Formula: C21H19FN6O2
Molecular weight: 406.413
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: PF-06463922 is a novel, orally available, CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. IC50 value: <0.02 nM/<0.07 nM/0.7 nM(Ki, ROS1/ALK (WT)/ALK (L1196M)) [1] Target: ALK/ROS1 dual inhibitor in vitro: PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM [1]. PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the crizotinib-refractory ROS1(G2032R) mutation and the ROS1(G2026M) gatekeeper mutation. Compared with crizotinib and the second-generation ALK/ROS1 inhibitors ceritinib and alectinib, PF-06463922 showed significantly improved inhibitory activity against ROS1 kinase [2]. in vivo: PF-06463922 showed marked antitumor activity in tumor models expressing FIG-ROS1, CD74-ROS1, and the CD74-ROS1(G2032R) mutation. Furthermore, PF-06463922 demonstrated antitumor activity in a genetically engineered mouse model of FIG-ROS1 glioblastoma [2].
Safety information: 
Additional information: 
Synonyms: HY-12215; Lorlatinib; PF 06463922; PF06463922
Multi-dimensional genomic analysis of myoepithelial carcinoma identifies prevalent oncogenic gene fusions', Martin Dalin, . Nat Commun. 2017 Oct 30;8(1):1197. Read more